Glibenclamide Nanocrystals in a Biodegradable Chitosan Patch for Transdermal Delivery: Engineering, Formulation, and Evaluation

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• 作者：Hany S.M. Ali¹ ; ² ; ^{hsali@taibahu.edu.sa} ; ^{hafandy2000@yahoo.com} ; Ahmed F. Hanafy¹ ; ³ ; ^{akorayem@yahoo.com} ; ^{drafathy@gmail.com}
• 关键词：nanoparticles ; transdermal delivery systems ; chitosan ; pharmacodynamics ; permeability
• 刊名：Journal of Pharmaceutical Sciences
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：106
• 期：1
• 页码：402-410
• 全文大小：2427 K
• 卷排序：106

文摘

Glibenclamide (GBD) nanocrystals (D50 = 429 nm) were engineered by applying combined precipitation and homogenization procedures. GBD crystallinity was maintained during the nanonization process as revealed by differential scanning calorimetry and X-ray analyses. Nanonized and micronized GBD were incorporated into chitosan solutions to fabricate transdermal delivery systems (TDDSs), nano- and micro-GBD, respectively. The fabricated TDDSs displayed satisfactory physicochemical characteristics without substantial aggregation of GBD nanocrystals during the casting and drying procedures. Within 24 hours, about 85 ± 3.1% of the GBD content was released from nano-GBD, compared to 61 ± 3.9% from micro-GBD. Cumulative permeation of GBD from nano-GBD after 24 hours was 498 ± 33.35 compared to 362 ± 25.25 μg/cm2 from micro-GBD. The calculated flux across rat skin for nano-GBD was 23.14 compared to 13.64 μg/cm2/h for micro-GBD, with an enhancement factor of 1.7. In vivo assessment clearly revealed the enhanced efficacy of nano-GBD to reduce blood glucose levels and counteract the induced hyperglycemia in tested animals compared to micro-GBD (p < 0.5). Simultaneously, the nano-GBD was able to maintain higher drug concentration for longer time (24 hours, p < 0.5) and minimize intense action and hypoglycemia associated with GBD oral therapy (p < 0.5).