Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats

The cellulose-based polymers are extensively employed in oral formulations for addressing ADMET issues of API. Herein, we report the synergistic effect of hydroxyethyl cellulose in solubility/dissolution enhancement of BCS class II, anthelmintic drug niclosamide. The low solubility and poor oral bio...
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Gespeichert in:

Autor*in:	Bhanushali, Jigar S. [verfasserIn] Dhiman, Sumit [verfasserIn] Nandi, Utpal [verfasserIn] Bharate, Sonali S. [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2022

Schlagwörter:	Hydroxyethyl cellulose Niclosamide Binary and ternary solid dispersions Molecular interactions Enhanced dissolution Oral pharmacokinetics

Übergeordnetes Werk:	Enthalten in: International journal of pharmaceutics - New York, NY [u.a.] : Elsevier, 1978, 626
Übergeordnetes Werk:	volume:626

DOI / URN:	10.1016/j.ijpharm.2022.122144

Katalog-ID:	ELV008514690

Internformat


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520			\|a The cellulose-based polymers are extensively employed in oral formulations for addressing ADMET issues of API. Herein, we report the synergistic effect of hydroxyethyl cellulose in solubility/dissolution enhancement of BCS class II, anthelmintic drug niclosamide. The low solubility and poor oral bioavailability are the primary reasons for its high daily dose. The amorphous solid dispersions (ASDs) developed herein demonstrated reproducible solubility and dissolution enhancement in smaller-to-pilot batches. The significant boost in niclosamide solubility in HEC-based binary SD was rationalized as a result of intermolecular H-bonding as indicated by in-silico studies and further supported by characterization data. HEC is plausibly inhibiting the precipitation of drug and thereby enabling high dissolution and permeation across the membrane. The comparative oral pharmacokinetics in Wistar rats at 25 mg/kg provided 4.4-fold higher plasma exposure of niclosamide in SD formulation SB-ASD-N2 over the plain drug. The results presented herein warrant validation of this ASD under clinical settings.
650		4	\|a Hydroxyethyl cellulose
650		4	\|a Niclosamide
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matchkey_str	article:18733476:2022----::oeuaitrcinoncoaieihyrxehlellsibnradenraoposoidsesososnritcnacmno
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publishDate	2022
allfields	10.1016/j.ijpharm.2022.122144 doi (DE-627)ELV008514690 (ELSEVIER)S0378-5173(22)00697-4 DE-627 ger DE-627 rda eng 610 VZ 15,3 ssgn PHARM DE-84 fid 44.40 bkl Bhanushali, Jigar S. verfasserin aut Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats 2022 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The cellulose-based polymers are extensively employed in oral formulations for addressing ADMET issues of API. Herein, we report the synergistic effect of hydroxyethyl cellulose in solubility/dissolution enhancement of BCS class II, anthelmintic drug niclosamide. The low solubility and poor oral bioavailability are the primary reasons for its high daily dose. The amorphous solid dispersions (ASDs) developed herein demonstrated reproducible solubility and dissolution enhancement in smaller-to-pilot batches. The significant boost in niclosamide solubility in HEC-based binary SD was rationalized as a result of intermolecular H-bonding as indicated by in-silico studies and further supported by characterization data. HEC is plausibly inhibiting the precipitation of drug and thereby enabling high dissolution and permeation across the membrane. The comparative oral pharmacokinetics in Wistar rats at 25 mg/kg provided 4.4-fold higher plasma exposure of niclosamide in SD formulation SB-ASD-N2 over the plain drug. The results presented herein warrant validation of this ASD under clinical settings. Hydroxyethyl cellulose Niclosamide Binary and ternary solid dispersions Molecular interactions Enhanced dissolution Oral pharmacokinetics Dhiman, Sumit verfasserin aut Nandi, Utpal verfasserin aut Bharate, Sonali S. verfasserin aut Enthalten in International journal of pharmaceutics New York, NY [u.a.] : Elsevier, 1978 626 Online-Ressource (DE-627)301512817 (DE-600)1484643-3 (DE-576)081952708 1873-3476 nnns volume:626 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_224 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2038 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2336 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4313 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4338 GBV_ILN_4393 44.40 Pharmazie Pharmazeutika VZ AR 626
spelling	10.1016/j.ijpharm.2022.122144 doi (DE-627)ELV008514690 (ELSEVIER)S0378-5173(22)00697-4 DE-627 ger DE-627 rda eng 610 VZ 15,3 ssgn PHARM DE-84 fid 44.40 bkl Bhanushali, Jigar S. verfasserin aut Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats 2022 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The cellulose-based polymers are extensively employed in oral formulations for addressing ADMET issues of API. Herein, we report the synergistic effect of hydroxyethyl cellulose in solubility/dissolution enhancement of BCS class II, anthelmintic drug niclosamide. The low solubility and poor oral bioavailability are the primary reasons for its high daily dose. The amorphous solid dispersions (ASDs) developed herein demonstrated reproducible solubility and dissolution enhancement in smaller-to-pilot batches. The significant boost in niclosamide solubility in HEC-based binary SD was rationalized as a result of intermolecular H-bonding as indicated by in-silico studies and further supported by characterization data. HEC is plausibly inhibiting the precipitation of drug and thereby enabling high dissolution and permeation across the membrane. The comparative oral pharmacokinetics in Wistar rats at 25 mg/kg provided 4.4-fold higher plasma exposure of niclosamide in SD formulation SB-ASD-N2 over the plain drug. The results presented herein warrant validation of this ASD under clinical settings. Hydroxyethyl cellulose Niclosamide Binary and ternary solid dispersions Molecular interactions Enhanced dissolution Oral pharmacokinetics Dhiman, Sumit verfasserin aut Nandi, Utpal verfasserin aut Bharate, Sonali S. verfasserin aut Enthalten in International journal of pharmaceutics New York, NY [u.a.] : Elsevier, 1978 626 Online-Ressource (DE-627)301512817 (DE-600)1484643-3 (DE-576)081952708 1873-3476 nnns volume:626 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_224 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2038 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2336 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4313 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4338 GBV_ILN_4393 44.40 Pharmazie Pharmazeutika VZ AR 626
allfields_unstemmed	10.1016/j.ijpharm.2022.122144 doi (DE-627)ELV008514690 (ELSEVIER)S0378-5173(22)00697-4 DE-627 ger DE-627 rda eng 610 VZ 15,3 ssgn PHARM DE-84 fid 44.40 bkl Bhanushali, Jigar S. verfasserin aut Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats 2022 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The cellulose-based polymers are extensively employed in oral formulations for addressing ADMET issues of API. Herein, we report the synergistic effect of hydroxyethyl cellulose in solubility/dissolution enhancement of BCS class II, anthelmintic drug niclosamide. The low solubility and poor oral bioavailability are the primary reasons for its high daily dose. The amorphous solid dispersions (ASDs) developed herein demonstrated reproducible solubility and dissolution enhancement in smaller-to-pilot batches. The significant boost in niclosamide solubility in HEC-based binary SD was rationalized as a result of intermolecular H-bonding as indicated by in-silico studies and further supported by characterization data. HEC is plausibly inhibiting the precipitation of drug and thereby enabling high dissolution and permeation across the membrane. The comparative oral pharmacokinetics in Wistar rats at 25 mg/kg provided 4.4-fold higher plasma exposure of niclosamide in SD formulation SB-ASD-N2 over the plain drug. The results presented herein warrant validation of this ASD under clinical settings. Hydroxyethyl cellulose Niclosamide Binary and ternary solid dispersions Molecular interactions Enhanced dissolution Oral pharmacokinetics Dhiman, Sumit verfasserin aut Nandi, Utpal verfasserin aut Bharate, Sonali S. verfasserin aut Enthalten in International journal of pharmaceutics New York, NY [u.a.] : Elsevier, 1978 626 Online-Ressource (DE-627)301512817 (DE-600)1484643-3 (DE-576)081952708 1873-3476 nnns volume:626 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_224 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2038 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2336 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4313 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4338 GBV_ILN_4393 44.40 Pharmazie Pharmazeutika VZ AR 626
allfieldsGer	10.1016/j.ijpharm.2022.122144 doi (DE-627)ELV008514690 (ELSEVIER)S0378-5173(22)00697-4 DE-627 ger DE-627 rda eng 610 VZ 15,3 ssgn PHARM DE-84 fid 44.40 bkl Bhanushali, Jigar S. verfasserin aut Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats 2022 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The cellulose-based polymers are extensively employed in oral formulations for addressing ADMET issues of API. Herein, we report the synergistic effect of hydroxyethyl cellulose in solubility/dissolution enhancement of BCS class II, anthelmintic drug niclosamide. The low solubility and poor oral bioavailability are the primary reasons for its high daily dose. The amorphous solid dispersions (ASDs) developed herein demonstrated reproducible solubility and dissolution enhancement in smaller-to-pilot batches. The significant boost in niclosamide solubility in HEC-based binary SD was rationalized as a result of intermolecular H-bonding as indicated by in-silico studies and further supported by characterization data. HEC is plausibly inhibiting the precipitation of drug and thereby enabling high dissolution and permeation across the membrane. The comparative oral pharmacokinetics in Wistar rats at 25 mg/kg provided 4.4-fold higher plasma exposure of niclosamide in SD formulation SB-ASD-N2 over the plain drug. The results presented herein warrant validation of this ASD under clinical settings. Hydroxyethyl cellulose Niclosamide Binary and ternary solid dispersions Molecular interactions Enhanced dissolution Oral pharmacokinetics Dhiman, Sumit verfasserin aut Nandi, Utpal verfasserin aut Bharate, Sonali S. verfasserin aut Enthalten in International journal of pharmaceutics New York, NY [u.a.] : Elsevier, 1978 626 Online-Ressource (DE-627)301512817 (DE-600)1484643-3 (DE-576)081952708 1873-3476 nnns volume:626 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_224 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2038 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2336 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4313 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4338 GBV_ILN_4393 44.40 Pharmazie Pharmazeutika VZ AR 626
allfieldsSound	10.1016/j.ijpharm.2022.122144 doi (DE-627)ELV008514690 (ELSEVIER)S0378-5173(22)00697-4 DE-627 ger DE-627 rda eng 610 VZ 15,3 ssgn PHARM DE-84 fid 44.40 bkl Bhanushali, Jigar S. verfasserin aut Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats 2022 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The cellulose-based polymers are extensively employed in oral formulations for addressing ADMET issues of API. Herein, we report the synergistic effect of hydroxyethyl cellulose in solubility/dissolution enhancement of BCS class II, anthelmintic drug niclosamide. The low solubility and poor oral bioavailability are the primary reasons for its high daily dose. The amorphous solid dispersions (ASDs) developed herein demonstrated reproducible solubility and dissolution enhancement in smaller-to-pilot batches. The significant boost in niclosamide solubility in HEC-based binary SD was rationalized as a result of intermolecular H-bonding as indicated by in-silico studies and further supported by characterization data. HEC is plausibly inhibiting the precipitation of drug and thereby enabling high dissolution and permeation across the membrane. The comparative oral pharmacokinetics in Wistar rats at 25 mg/kg provided 4.4-fold higher plasma exposure of niclosamide in SD formulation SB-ASD-N2 over the plain drug. The results presented herein warrant validation of this ASD under clinical settings. Hydroxyethyl cellulose Niclosamide Binary and ternary solid dispersions Molecular interactions Enhanced dissolution Oral pharmacokinetics Dhiman, Sumit verfasserin aut Nandi, Utpal verfasserin aut Bharate, Sonali S. verfasserin aut Enthalten in International journal of pharmaceutics New York, NY [u.a.] : Elsevier, 1978 626 Online-Ressource (DE-627)301512817 (DE-600)1484643-3 (DE-576)081952708 1873-3476 nnns volume:626 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_224 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2038 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2336 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4313 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4338 GBV_ILN_4393 44.40 Pharmazie Pharmazeutika VZ AR 626
language	English
source	Enthalten in International journal of pharmaceutics 626 volume:626
sourceStr	Enthalten in International journal of pharmaceutics 626 volume:626
format_phy_str_mv	Article
bklname	Pharmazie Pharmazeutika
institution	findex.gbv.de
topic_facet	Hydroxyethyl cellulose Niclosamide Binary and ternary solid dispersions Molecular interactions Enhanced dissolution Oral pharmacokinetics
dewey-raw	610
isfreeaccess_bool	false
container_title	International journal of pharmaceutics
authorswithroles_txt_mv	Bhanushali, Jigar S. @@aut@@ Dhiman, Sumit @@aut@@ Nandi, Utpal @@aut@@ Bharate, Sonali S. @@aut@@
publishDateDaySort_date	2022-01-01T00:00:00Z
hierarchy_top_id	301512817
dewey-sort	3610
id	ELV008514690
language_de	englisch
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author	Bhanushali, Jigar S.
spellingShingle	Bhanushali, Jigar S. ddc 610 ssgn 15,3 fid PHARM bkl 44.40 misc Hydroxyethyl cellulose misc Niclosamide misc Binary and ternary solid dispersions misc Molecular interactions misc Enhanced dissolution misc Oral pharmacokinetics Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats
authorStr	Bhanushali, Jigar S.
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topic_title	610 VZ 15,3 ssgn PHARM DE-84 fid 44.40 bkl Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats Hydroxyethyl cellulose Niclosamide Binary and ternary solid dispersions Molecular interactions Enhanced dissolution Oral pharmacokinetics
topic	ddc 610 ssgn 15,3 fid PHARM bkl 44.40 misc Hydroxyethyl cellulose misc Niclosamide misc Binary and ternary solid dispersions misc Molecular interactions misc Enhanced dissolution misc Oral pharmacokinetics
topic_unstemmed	ddc 610 ssgn 15,3 fid PHARM bkl 44.40 misc Hydroxyethyl cellulose misc Niclosamide misc Binary and ternary solid dispersions misc Molecular interactions misc Enhanced dissolution misc Oral pharmacokinetics
topic_browse	ddc 610 ssgn 15,3 fid PHARM bkl 44.40 misc Hydroxyethyl cellulose misc Niclosamide misc Binary and ternary solid dispersions misc Molecular interactions misc Enhanced dissolution misc Oral pharmacokinetics
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title	Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats
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title_full	Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats
author_sort	Bhanushali, Jigar S.
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author_browse	Bhanushali, Jigar S. Dhiman, Sumit Nandi, Utpal Bharate, Sonali S.
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author-letter	Bhanushali, Jigar S.
doi_str_mv	10.1016/j.ijpharm.2022.122144
dewey-full	610
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title_sort	molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats
title_auth	Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats
abstract	The cellulose-based polymers are extensively employed in oral formulations for addressing ADMET issues of API. Herein, we report the synergistic effect of hydroxyethyl cellulose in solubility/dissolution enhancement of BCS class II, anthelmintic drug niclosamide. The low solubility and poor oral bioavailability are the primary reasons for its high daily dose. The amorphous solid dispersions (ASDs) developed herein demonstrated reproducible solubility and dissolution enhancement in smaller-to-pilot batches. The significant boost in niclosamide solubility in HEC-based binary SD was rationalized as a result of intermolecular H-bonding as indicated by in-silico studies and further supported by characterization data. HEC is plausibly inhibiting the precipitation of drug and thereby enabling high dissolution and permeation across the membrane. The comparative oral pharmacokinetics in Wistar rats at 25 mg/kg provided 4.4-fold higher plasma exposure of niclosamide in SD formulation SB-ASD-N2 over the plain drug. The results presented herein warrant validation of this ASD under clinical settings.
abstractGer	The cellulose-based polymers are extensively employed in oral formulations for addressing ADMET issues of API. Herein, we report the synergistic effect of hydroxyethyl cellulose in solubility/dissolution enhancement of BCS class II, anthelmintic drug niclosamide. The low solubility and poor oral bioavailability are the primary reasons for its high daily dose. The amorphous solid dispersions (ASDs) developed herein demonstrated reproducible solubility and dissolution enhancement in smaller-to-pilot batches. The significant boost in niclosamide solubility in HEC-based binary SD was rationalized as a result of intermolecular H-bonding as indicated by in-silico studies and further supported by characterization data. HEC is plausibly inhibiting the precipitation of drug and thereby enabling high dissolution and permeation across the membrane. The comparative oral pharmacokinetics in Wistar rats at 25 mg/kg provided 4.4-fold higher plasma exposure of niclosamide in SD formulation SB-ASD-N2 over the plain drug. The results presented herein warrant validation of this ASD under clinical settings.
abstract_unstemmed	The cellulose-based polymers are extensively employed in oral formulations for addressing ADMET issues of API. Herein, we report the synergistic effect of hydroxyethyl cellulose in solubility/dissolution enhancement of BCS class II, anthelmintic drug niclosamide. The low solubility and poor oral bioavailability are the primary reasons for its high daily dose. The amorphous solid dispersions (ASDs) developed herein demonstrated reproducible solubility and dissolution enhancement in smaller-to-pilot batches. The significant boost in niclosamide solubility in HEC-based binary SD was rationalized as a result of intermolecular H-bonding as indicated by in-silico studies and further supported by characterization data. HEC is plausibly inhibiting the precipitation of drug and thereby enabling high dissolution and permeation across the membrane. The comparative oral pharmacokinetics in Wistar rats at 25 mg/kg provided 4.4-fold higher plasma exposure of niclosamide in SD formulation SB-ASD-N2 over the plain drug. The results presented herein warrant validation of this ASD under clinical settings.
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title_short	Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats
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author2	Dhiman, Sumit Nandi, Utpal Bharate, Sonali S.
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up_date	2024-07-06T19:57:44.436Z
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Molecular interactions of niclosamide with hydroxyethyl cellulose in binary and ternary amorphous solid dispersions for synergistic enhancement of water solubility and oral pharmacokinetics in rats

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