Design and Development of Nanoparticles Containing α-Mangostin for Wound Application

Peerapat Chidchai, Kanokwan Singpanna, Kamonchai Ketduang, Aristarn Uamjan, Prasopchai Patrojanasophon, Chaiyakarn Pornpitchanarong
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Abstract

Objective: The objective of this research was to design and develop nanoparticles containing α-mangostin (α-MG) for wound applications. Material and Methods: The nanoparticles were composed of polycaprolactone (PCL) and Eudragit® S 100 (EDG), with 10% wt of α-MG; wherein, the optimal compositions of the nanoparticles were studied using a mixture-typed simplex lattice design. The amount of PCL (5-20 milligram/milliliter (mg/mL)) and EDG (5-20 mg/mL) were varied, and the effects of the components toward particle size, size distribution, zeta potential; drug content, and drug release were examined. The physicochemical properties of the nanoparticles were analyzed using a zetasizer. The content of α-MG was quantified using High Pressure Liquid Chromatography. Results: It was found that the nanoparticles having different mixtures of PCL and EDG did not affect the physicochemical properties nor the drug content. However, the release of α-MG can be tuned by varying the nanoparticle composition. Formulations with higher EDG showed greater drug release at pH 7.4, because of the polymer dissolution at a specified pH. The composition of the optimized formulation composed of 16.5 mg/mL of EDG and 8.5 mg/mL of PCL. The optimized nanoparticle showed a controlled release profile of up to 12 h, which was superior to the α-MG solution. Conclusion: The developed nanoparticles of PCL and EDG can be considered as a promising platform to deliver α-MG for wound applications.
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伤口用α-山竹苷纳米颗粒的设计与研制
目的:设计并制备用于伤口创面的α-山竹苷纳米颗粒。材料与方法:纳米颗粒由聚己内酯(PCL)和Eudragit®s100 (EDG)组成,α-MG质量分数为10%;其中,采用混合型单纯形晶格设计研究了纳米颗粒的最佳组成。PCL (5 ~ 20 mg/mL)和EDG (5 ~ 20 mg/mL)的添加量不同,组分对粒径、粒径分布、zeta电位的影响也不同;测定药物含量和释放度。用热还原仪分析了纳米颗粒的物理化学性质。采用高压液相色谱法测定α-MG的含量。结果:不同PCL和EDG的混合对纳米颗粒的理化性质和药物含量均无影响。然而,α-MG的释放可以通过改变纳米颗粒的组成来调节。EDG越高的制剂在pH值为7.4时的释药效果越好,这是由于聚合物在特定pH下的溶解作用。优化后的制剂由16.5 mg/mL EDG和8.5 mg/mL PCL组成。优化后的纳米颗粒的缓释时间长达12 h,优于α-MG溶液。结论:制备的PCL和EDG纳米颗粒可作为α-MG在创面上的应用平台。
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