Formulation and comparative in vitro evaluation of various dexamethasone-loaded pH-sensitive polymeric nanoparticles intended for dermal applications

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• 作者：Fitsum Feleke Sahle^a ; Christian Gerecke^b ; Burkhard Kleuser^b ; Roland Bodmeier^a ; ^{bodmeier@zedat.fu-berlin.de}
• 关键词：Dexamethasone (PubChem CID ; 5743) ; Eudragits (PubChem CID ; 65358) ; HPMCP (PubChem CID ; 57469) ; Cellulose acetate phthalate (PubChem CID ; 44135440) ; Polyvinyl alcohol (PubChem CID ; 11199) ; MTT (PubChem CID ; 64965) ; H2DCFDA (PubChem CID ; 77718) ; Acetic acid (PubChem CID ; 176) ; Potassium dihydrogen phosphate (PubChem CID ; 516951)
• 刊名：International Journal of Pharmaceutics
• 出版年：2017
• 出版时间：10 January 2017
• 年：2017
• 卷：516
• 期：1-2
• 页码：21-31
• 全文大小：3760 K
• 卷排序：516

文摘

pH-sensitive nanoparticles have a great potential for dermal and transfollicular drug delivery. In this study, pH-sensitive, dexamethasone-loaded Eudragit® L 100, Eudragit® L 100-55, Eudragit® S 100, HPMCP-50, HPMCP-55 and cellulose acetate phthalate nanoparticles were prepared by nanoprecipitation and characterized. The pH-dependent swelling, erosion, dissolution and drug release kinetics were investigated in vitro using dynamic light scattering and Franz diffusion cells, respectively. Their toxicity potential was assessed by the ROS and MTT assays. 100–700 nm nanoparticles with high drug loading and entrapment efficiency were obtained. The nanoparticles bear no toxicity potential. Cellulose phthalates nanoparticles were more sensitive to pH than acrylates nanoparticles. They dissolved in 10 mM pH 7.5 buffer and released > 80% of the drug within 7 h. The acrylate nanoparticles dissolved in 40 mM pH 7.5 buffer and released 65–70% of the drug within 7 h. The nanoparticles remained intact in 10 and 40 mM pH 6.0 buffers (HPMCP nanoparticles dissolved in 40 mM pH 6.0 buffer) and released slowly. The nanoparticles properties could be modulated by blending the different polymers. In conclusion, various pH-sensitive nanoparticles that could release differently on the skin surface and dissolve and release in the hair follicles were obtained.