Liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs
Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
Aloisio, Carolina [verfasserIn] |
|---|
| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2017transfer abstract |
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| Umfang: |
8 |
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| Übergeordnetes Werk: |
Enthalten in: Application of a fuzzy-logic based model for risk assessment in additive manufacturing R&D projects - Moreno-Cabezali, Belen Maria ELSEVIER, 2020, an international journal devoted to fundamental aspects of structure, interactions and dynamic processes in simple, molecular and complex liquids, New York, NY [u.a.] |
|---|---|
| Übergeordnetes Werk: |
volume:229 ; year:2017 ; pages:106-113 ; extent:8 |
| Links: |
|---|
| DOI / URN: |
10.1016/j.molliq.2016.12.035 |
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| 245 | 1 | 0 | |a Liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs |
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| 520 | |a Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. | ||
| 520 | |a Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. | ||
| 700 | 1 | |a Antimisiaris, Sophia G. |4 oth | |
| 700 | 1 | |a Longhi, Marcela R. |4 oth | |
| 773 | 0 | 8 | |i Enthalten in |n Elsevier |a Moreno-Cabezali, Belen Maria ELSEVIER |t Application of a fuzzy-logic based model for risk assessment in additive manufacturing R&D projects |d 2020 |d an international journal devoted to fundamental aspects of structure, interactions and dynamic processes in simple, molecular and complex liquids |g New York, NY [u.a.] |w (DE-627)ELV004280490 |
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10.1016/j.molliq.2016.12.035 doi GBVA2017004000010.pica (DE-627)ELV014843773 (ELSEVIER)S0167-7322(16)32329-7 DE-627 ger DE-627 rakwb eng 540 540 DE-600 004 VZ 85.35 bkl 54.80 bkl Aloisio, Carolina verfasserin aut Liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs 2017transfer abstract 8 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. Antimisiaris, Sophia G. oth Longhi, Marcela R. oth Enthalten in Elsevier Moreno-Cabezali, Belen Maria ELSEVIER Application of a fuzzy-logic based model for risk assessment in additive manufacturing R&D projects 2020 an international journal devoted to fundamental aspects of structure, interactions and dynamic processes in simple, molecular and complex liquids New York, NY [u.a.] (DE-627)ELV004280490 volume:229 year:2017 pages:106-113 extent:8 https://doi.org/10.1016/j.molliq.2016.12.035 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 85.35 Fertigung VZ 54.80 Angewandte Informatik VZ AR 229 2017 106-113 8 045F 540 |
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10.1016/j.molliq.2016.12.035 doi GBVA2017004000010.pica (DE-627)ELV014843773 (ELSEVIER)S0167-7322(16)32329-7 DE-627 ger DE-627 rakwb eng 540 540 DE-600 004 VZ 85.35 bkl 54.80 bkl Aloisio, Carolina verfasserin aut Liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs 2017transfer abstract 8 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. Antimisiaris, Sophia G. oth Longhi, Marcela R. oth Enthalten in Elsevier Moreno-Cabezali, Belen Maria ELSEVIER Application of a fuzzy-logic based model for risk assessment in additive manufacturing R&D projects 2020 an international journal devoted to fundamental aspects of structure, interactions and dynamic processes in simple, molecular and complex liquids New York, NY [u.a.] (DE-627)ELV004280490 volume:229 year:2017 pages:106-113 extent:8 https://doi.org/10.1016/j.molliq.2016.12.035 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 85.35 Fertigung VZ 54.80 Angewandte Informatik VZ AR 229 2017 106-113 8 045F 540 |
| allfields_unstemmed |
10.1016/j.molliq.2016.12.035 doi GBVA2017004000010.pica (DE-627)ELV014843773 (ELSEVIER)S0167-7322(16)32329-7 DE-627 ger DE-627 rakwb eng 540 540 DE-600 004 VZ 85.35 bkl 54.80 bkl Aloisio, Carolina verfasserin aut Liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs 2017transfer abstract 8 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. Antimisiaris, Sophia G. oth Longhi, Marcela R. oth Enthalten in Elsevier Moreno-Cabezali, Belen Maria ELSEVIER Application of a fuzzy-logic based model for risk assessment in additive manufacturing R&D projects 2020 an international journal devoted to fundamental aspects of structure, interactions and dynamic processes in simple, molecular and complex liquids New York, NY [u.a.] (DE-627)ELV004280490 volume:229 year:2017 pages:106-113 extent:8 https://doi.org/10.1016/j.molliq.2016.12.035 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 85.35 Fertigung VZ 54.80 Angewandte Informatik VZ AR 229 2017 106-113 8 045F 540 |
| allfieldsGer |
10.1016/j.molliq.2016.12.035 doi GBVA2017004000010.pica (DE-627)ELV014843773 (ELSEVIER)S0167-7322(16)32329-7 DE-627 ger DE-627 rakwb eng 540 540 DE-600 004 VZ 85.35 bkl 54.80 bkl Aloisio, Carolina verfasserin aut Liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs 2017transfer abstract 8 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. Antimisiaris, Sophia G. oth Longhi, Marcela R. oth Enthalten in Elsevier Moreno-Cabezali, Belen Maria ELSEVIER Application of a fuzzy-logic based model for risk assessment in additive manufacturing R&D projects 2020 an international journal devoted to fundamental aspects of structure, interactions and dynamic processes in simple, molecular and complex liquids New York, NY [u.a.] (DE-627)ELV004280490 volume:229 year:2017 pages:106-113 extent:8 https://doi.org/10.1016/j.molliq.2016.12.035 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 85.35 Fertigung VZ 54.80 Angewandte Informatik VZ AR 229 2017 106-113 8 045F 540 |
| allfieldsSound |
10.1016/j.molliq.2016.12.035 doi GBVA2017004000010.pica (DE-627)ELV014843773 (ELSEVIER)S0167-7322(16)32329-7 DE-627 ger DE-627 rakwb eng 540 540 DE-600 004 VZ 85.35 bkl 54.80 bkl Aloisio, Carolina verfasserin aut Liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs 2017transfer abstract 8 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. Antimisiaris, Sophia G. oth Longhi, Marcela R. oth Enthalten in Elsevier Moreno-Cabezali, Belen Maria ELSEVIER Application of a fuzzy-logic based model for risk assessment in additive manufacturing R&D projects 2020 an international journal devoted to fundamental aspects of structure, interactions and dynamic processes in simple, molecular and complex liquids New York, NY [u.a.] (DE-627)ELV004280490 volume:229 year:2017 pages:106-113 extent:8 https://doi.org/10.1016/j.molliq.2016.12.035 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 85.35 Fertigung VZ 54.80 Angewandte Informatik VZ AR 229 2017 106-113 8 045F 540 |
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Enthalten in Application of a fuzzy-logic based model for risk assessment in additive manufacturing R&D projects New York, NY [u.a.] volume:229 year:2017 pages:106-113 extent:8 |
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Enthalten in Application of a fuzzy-logic based model for risk assessment in additive manufacturing R&D projects New York, NY [u.a.] volume:229 year:2017 pages:106-113 extent:8 |
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liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs |
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Liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs |
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Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. |
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Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. |
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Poorly soluble drug-loaded liposomes are well known for their ability to solubilize and improve the bioavailability of the carried molecules, and may provide benefits as oral drug delivery systems. In this work, we aim to evaluate the effect of the incorporation of β-cyclodextrin (βCD), methyl-βCD (MβCD), hydroxypropil-βCD (HPβCD) and meglumine (MEG) in liposomes for the oral delivery of the poorly water-soluble drugs, sulfamerazine (SMR) and indomethacin (INM). Liposomes with egg phosphatidylcholine (PC) and cholesterol (CHO), incorporating SMR or INM as plain drug or inclusion complexes, were prepared using the thin film hydration method or dehydration-rehydration method, respectively. The systems were characterized by particle size, polydispersity and zeta potential measurements, and drug-component interaction studies were performed by 1H NMR. Liposome stability in presence of SMR, INM, CD and MEG was determined by the retention of vesicle encapsulated calcein after incubation in solutions of pH7.4, at 37°C for up to 48h. Drug entrapment, as well as drug release, were estimated for all liposome types prepared. The 1H NMR studies revealed that the drugs presented interaction with lipids of the liposomes, suggesting the location of the drugs in the lipid bilayer. The liposomes presented high stability in the presence of the drugs, βCD, HPβCD or MEG. The highest entrapment values were achieved for SMR and INM with PC:CHO 3:1 liposomes when MEG and HPβCD were used, respectively (5636.28 and 439.54mmol/mol), meaning that 18 and 43 times higher incorporation of SMR and INM were achieved in comparison with the ligand-free formulation. The in-vitro release studies showed a strong influence of the ligands on the delivery of the drugs from the liposomes. |
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