Response surface optimization of biocompatible elastic nanovesicles loaded with rosuvastatin calcium: enhanced bioavaila
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ORIGINAL ARTICLE
Response surface optimization of biocompatible elastic nanovesicles loaded with rosuvastatin calcium: enhanced bioavailability and anticancer efficacy Ibrahim Elsayed 1,2 & Rania Moataz El-Dahmy 3 & Soad Z. El-Emam 4 & Ahmed Hassen Elshafeey 1 & Nabaweya Abdelaziz Abd El Gawad 3 & Omaima Naim El-Gazayerly 1
# Controlled Release Society 2020
Abstract Statins are mainly used for the treatment of hyperlipidemia, but recently, their anticancer role was extremely investigated. The goal of this study was to statistically optimize novel elastic nanovesicles containing rosuvastatin calcium to improve its transdermal permeability, bioavailability, and anticancer effect. The elastic nanovesicles were composed of Tween® 80, cetyl alcohol, and clove oil. The nanodispersions were investigated for their entrapment efficiency, particle size, zeta potential, polydispersity index, and elasticity. The optimized elastic nanovesicular dispersion is composed of 20% cetyl alcohol, 53.47% Tween 80, and 26.53% clove oil. Carboxy methylcellulose was utilized to convert the optimized elastic nanovesicular dispersion into elastic nanovesicular gels. Both the optimized dispersion and the optimized gel (containing 2% w/v carboxymethylcellulose) were subjected to in vitro release study, scanning and transmission electron microscopy, histopathological evaluation, and ex vivo permeation. The cell viability assay of the optimized gel on MCF-7 and Hela cell lines showed significant antiproliferative and potent cytotoxic effects when compared to the drug gel. Moreover, the optimized gel accomplished a significant increase in rosuvastatin bioavailability upon comparison with the drug gel. The optimized gel could be considered as a promising nanocarrier for statins transdermal delivery to increase their systemic bioavailability and anticancer effect.
Keywords Statins . Nanovesicles . Anticancer . Transdermal . Tween . Clove oil
Highlights • Rosuvastatin calcium was formulated in nanovesicles composed of cetyl alcohol, Tween 80, and clove oil. • The optimized nanodispersion was selected based on a simple lattice mixture experimental design. • The optimized nanodispersion was converted to gel using carboxy methylcellulose. • The nanostructed gel showed significantly higher ex vivo permeation, anticancer efficacy, and in vivo bioavailability when compared to the unformulated drug. • Consequently, the nanostructured gel could be considered as promising nanocarriers for transdermal drug delivery of rosuvastatin calcium. * Ibrahim Elsayed [email protected]; [email protected] 1
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt
2
Department of Pharmaceutical Sciences, College of Pharmacy, Gulf Medical University, Ajman, UAE
3
Department of Pharmaceutics, Faculty of Pharmacy, October 6 University, Cairo, Egypt
4
Department of Pharmacology and Toxicology, Faculty of Pharmacy, October 6 University, Cairo, Egypt
Drug Deliv. and Transl. Res.
Introduction Rosuva
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