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Tacrolimus-loaded lecithin-based nanostructured lipid carrier and nanoemulsion with propylene glycol monocaprylate as a liquid lipid: Formulation characterization and assessment of dermal delivery compared to referent ointment.
Savic, Vedrana; Ilic, Tanja; Nikolic, Ines; Markovic, Bojan; Calija, Bojan; Cekic, Nebojsa; Savic, Snezana.
Afiliación
  • Savic V; Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.
  • Ilic T; Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.
  • Nikolic I; Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.
  • Markovic B; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.
  • Calija B; Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.
  • Cekic N; Faculty of Technology, University of Nis, Leskovac, Serbia; DCP Hemigal, Leskovac, Serbia.
  • Savic S; Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia. Electronic address: snezana.savic@pharmacy.bg.ac.rs.
Int J Pharm ; 569: 118624, 2019 Oct 05.
Article en En | MEDLINE | ID: mdl-31419461
Nanostructured lipid carriers (NLC) and nanoemulsions (NE) are colloid carriers which could improve dermal delivery of tacrolimus. The aims of this study were to evaluate effects of different formulation and process parameters on physicochemical characteristics and stability of lecithin-based NLC with glyceryl palmitostearate as solid and propylene glycol monocaprylate as liquid lipid and to compare the influence of different inner structure of tacrolimus-loaded NLC and corresponding NE on physicochemical characteristics, stability, entrapment efficiency, in vitro drug release and overall skin performance. Solid/liquid lipid ratio, total amount of lipids, homogenization pressure and cooling after the preparation were identified as critical variables in NLC development. Moreover, tacrolimus-loaded NLC emerged as more stabile carrier than NE. Differential stripping performed on porcine ear skin revealed significantly higher tacrolimus amount in stratum corneum from nanocarriers compared to referent ointment (Protopic®). Similarly the highest amount of tacrolimus in hair follicles was obtained using NLC (268.54 ±â€¯92.38 ng/cm2), followed by NE (128.17 ±â€¯48.87 ng/cm2) and Protopic® (77.61 ±â€¯43.25 ng/cm2). Contrary, the highest permeation rate through full-thickness porcine ear skin was observed for Protopic®, implying that the selection of experimental setup is critical for reliable skin performance assessment. Overall, developed NLC could be suggested as promising carrier in a form of lotion for tacrolimus dermal delivery.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Portadores de Fármacos / Tacrolimus / Nanoestructuras / Lecitinas / Inmunosupresores Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Int J Pharm Año: 2019 Tipo del documento: Article Pais de publicación: Países Bajos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Portadores de Fármacos / Tacrolimus / Nanoestructuras / Lecitinas / Inmunosupresores Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Int J Pharm Año: 2019 Tipo del documento: Article Pais de publicación: Países Bajos