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Development and characterization of nano-emulsions and nano-emulgels for transdermal delivery of statins.
Sithole, Mduduzi N; Marais, Suzanne; Maree, Sumari M; Du Plessis, Lissinda H; Du Plessis, Jeanetta; Gerber, Minja.
Afiliación
  • Sithole MN; Centre of Excellence for Pharmaceutical Sciences (Pharmacen™), North-West University, Potchefstroom, South Africa.
  • Marais S; Afrigen Biologics (Pty) Limited, Formulation Development, Cape Town, South Africa.
  • Maree SM; Centre of Excellence for Pharmaceutical Sciences (Pharmacen™), North-West University, Potchefstroom, South Africa.
  • Du Plessis LH; Centre of Excellence for Pharmaceutical Sciences (Pharmacen™), North-West University, Potchefstroom, South Africa.
  • Du Plessis J; Centre of Excellence for Pharmaceutical Sciences (Pharmacen™), North-West University, Potchefstroom, South Africa.
  • Gerber M; Centre of Excellence for Pharmaceutical Sciences (Pharmacen™), North-West University, Potchefstroom, South Africa.
Expert Opin Drug Deliv ; 18(6): 789-801, 2021 06.
Article en En | MEDLINE | ID: mdl-33393386
BACKGROUND: Oral administration of statins for the treatment of familial hypercholesterolemia results in poor therapeutic outcomes and patient compliance. An alternative administration route is proposed to circumvent the current limitations. This research is aimed at developing nano-emulsions and nano-emulgels as the ultimate potential delivery systems of statins for administration via the transdermal route. METHODS: Oil-in-water (o/w) nano-formulations (nano-emulsions and nano-emulgels) containing 2% (w/w) of the selected statin and 8% apricot kernel oil as oil phase were formulated. The nano-formulations were characterized using transmission electron microscopy (TEM), pH, viscosity, droplet size and zeta-potential. RESULTS: Nano-emulsions' and nano-emulgels' droplet size ranged between 114.23-169.83 nm and 149.83-267.53 nm, respectively. The addition of Carbopol® Ultrez 20 increased the nano-emulsions' viscosity (3.59-8.38 cP) resulting in the formation of nano-emulgels (viscosity: 1911.00-46,090.00 cP). The entrapment efficiency (90.77-99.55%) confirmed the incorporation of the statins. Membrane release studies indicated that statins were released at higher flux values in nano-emulsions compared to their respective nano-emulgels. Ex vivo (skin diffusion) studies indicated higher median values in the nano-emulgels compared to their nano-emulsion counterparts. CONCLUSIONS: The results indicate the benefits of nano-emulsions and nano-emulgels as potential alternative delivery systems for the transdermal delivery of statins.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Hidroximetilglutaril-CoA Reductasas Límite: Humans Idioma: En Revista: Expert Opin Drug Deliv Asunto de la revista: FARMACOLOGIA / TERAPIA POR MEDICAMENTOS Año: 2021 Tipo del documento: Article País de afiliación: Sudáfrica Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Hidroximetilglutaril-CoA Reductasas Límite: Humans Idioma: En Revista: Expert Opin Drug Deliv Asunto de la revista: FARMACOLOGIA / TERAPIA POR MEDICAMENTOS Año: 2021 Tipo del documento: Article País de afiliación: Sudáfrica Pais de publicación: Reino Unido