Nanaki Stavroula G, Andrianidou Sophia, Barmpalexis Panagiotis, Christodoulou Evi, Bikiaris Dimitrios N
Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
Department of Pharmaceutical Technology, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
Polymers (Basel). 2021 May 11;13(10):1539. doi: 10.3390/polym13101539.
In the present study, the preparation of controlled-released leflunomide (LFD)-loaded skin patches was evaluated, utilizing the combination of chitosan (CS) nanoparticles (NPs) incorporated into suitable poly(l-lactic acid) (PLLA) or poly(lactic--glycolic acid) (PLGA) polyester matrices. Initially, LFD-loaded CS NPs of ~600 nm and a smooth surface were prepared, while strong inter-molecular interactions between the drug and the CS were unraveled. In the following step, the prepared LFD-loaded CS NPs were incorporated into PLLA or PLGA, and thin-film patches were prepared via spin-coating. Analysis of the prepared films showed that the incorporation of the drug-loaded CS NPs resulted in a significant increase in the drug's release rate and extent as compared to neat LFD-loaded polyester patches (i.e., prepared without the use of CS NPs). In-depth analysis of the prepared formulations showed that the amorphization of the drug within the matrix and the increased wetting properties of the prepared CS NPs were responsible for the improved thin-film patch characteristics.
在本研究中，通过将壳聚糖（CS）纳米颗粒（NPs）与合适的聚左旋乳酸（PLLA）或聚乳酸 - 乙醇酸共聚物（PLGA）聚酯基质相结合，对负载来氟米特（LFD）的控释皮肤贴片的制备进行了评估。首先，制备了粒径约600 nm且表面光滑的负载LFD的CS NPs，同时揭示了药物与CS之间强烈的分子间相互作用。接下来，将制备好的负载LFD的CS NPs掺入PLLA或PLGA中，并通过旋涂制备薄膜贴片。对制备的薄膜进行分析表明，与纯负载LFD的聚酯贴片（即不使用CS NPs制备的贴片）相比，掺入负载药物的CS NPs后，药物的释放速率和释放程度显著增加。对制备的制剂进行深入分析表明，基质中药物的非晶化以及制备的CS NPs润湿性的提高是薄膜贴片特性改善的原因。
