Efavirenz Loaded Mixed Polymeric Micelles: Formulation, Optimization, and <i>In Vitro</i> Characterization.

Madan, JR; Dere, SG; Awasthi, R; Dua, K

Efavirenz Loaded Mixed Polymeric Micelles: Formulation, Optimization, and <i>In Vitro</i> Characterization.

Madan, JR Dere, SG Awasthi, R Dua, K

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Publisher:: Mary Ann Liebert Inc
Publication Type:: Journal Article
Citation:: Assay and drug development technologies, 2021
Issue Date:: 2021-06-14

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Field	Value	Language
dc.contributor.author	Madan, JR
dc.contributor.author	Dere, SG
dc.contributor.author	Awasthi, R
dc.contributor.author	Dua, K https://orcid.org/0000-0002-7507-1159
dc.date.accessioned	2021-06-23T23:44:07Z
dc.date.available	2021-06-23T23:44:07Z
dc.date.issued	2021-06-14
dc.identifier.citation	Assay and drug development technologies, 2021
dc.identifier.issn	1540-658X
dc.identifier.issn	1557-8127
dc.identifier.uri	http://hdl.handle.net/10453/149736
dc.description.abstract	<i>Efavirenz (EFZ) is a biopharmaceutics classification system (BCS) Class-II, first-line antiretroviral (ARV) drug. However, its utility through the oral route is restricted by its poor solubility. The objective of this study was to formulate EFZ-loaded binary-mixed micelles as a potential carrier for oral administration of EFZ. Rubingh's regular solution theory was used to determine the interaction behavior of the two components (Cremophor RH 40 and Phospholipon 80H) and of the mixed micelles and synergistic behavior was confirmed. The mixed miceller system was formulated using solvent evaporation method and a 3<sup>2</sup> factorial design was used for the optimization of selected independent variables. Miceller systems were further characterized in terms of morphology, particle size, zeta potential, percent entrapment efficiency, and drug loading. Fourier transform infrared and differential scanning calorimetry measurements confirmed the entrapment of EFZ in the micelles. The optimized formulation presented desirable qualities viz., nanometric size (17.27 ± 0.079), high entrapment efficiency, and good colloidal stability. The prepared optimized micelles can be potential carriers for EFZ in ARV therapies.</i>
dc.format	Print-Electronic
dc.language	eng
dc.publisher	Mary Ann Liebert Inc
dc.relation.ispartof	Assay and drug development technologies
dc.relation.isbasedon	10.1089/adt.2021.027
dc.rights	info:eu-repo/semantics/closedAccess
dc.subject	0304 Medicinal and Biomolecular Chemistry, 0306 Physical Chemistry (incl. Structural), 1115 Pharmacology and Pharmaceutical Sciences
dc.subject.classification	Medicinal & Biomolecular Chemistry
dc.title	Efavirenz Loaded Mixed Polymeric Micelles: Formulation, Optimization, and <i>In Vitro</i> Characterization.
dc.type	Journal Article
utslib.location.activity	United States
utslib.for	0304 Medicinal and Biomolecular Chemistry
utslib.for	0306 Physical Chemistry (incl. Structural)
utslib.for	1115 Pharmacology and Pharmaceutical Sciences
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Faculty of Health
pubs.organisational-group	/University of Technology Sydney/Faculty of Health/Graduate School of Health
pubs.organisational-group	/University of Technology Sydney/Faculty of Health/Graduate School of Health/GSH.Pharmacy
utslib.copyright.status	closed_access	*
dc.date.updated	2021-06-23T23:44:05Z
pubs.publication-status	Published

Abstract:

Efavirenz (EFZ) is a biopharmaceutics classification system (BCS) Class-II, first-line antiretroviral (ARV) drug. However, its utility through the oral route is restricted by its poor solubility. The objective of this study was to formulate EFZ-loaded binary-mixed micelles as a potential carrier for oral administration of EFZ. Rubingh's regular solution theory was used to determine the interaction behavior of the two components (Cremophor RH 40 and Phospholipon 80H) and of the mixed micelles and synergistic behavior was confirmed. The mixed miceller system was formulated using solvent evaporation method and a 3² factorial design was used for the optimization of selected independent variables. Miceller systems were further characterized in terms of morphology, particle size, zeta potential, percent entrapment efficiency, and drug loading. Fourier transform infrared and differential scanning calorimetry measurements confirmed the entrapment of EFZ in the micelles. The optimized formulation presented desirable qualities viz., nanometric size (17.27 ± 0.079), high entrapment efficiency, and good colloidal stability. The prepared optimized micelles can be potential carriers for EFZ in ARV therapies.

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http://hdl.handle.net/10453/149736