Development, characterization and optimization of solid lipid nanoparticles of alpha-mangostin by central composite design approach

Q2 Pharmacology, Toxicology and Pharmaceutics
Vutti Nagendra Babu, G. S. N. K. Rao, Roja Rani Budha, R. R. Alavala, P. K. Desu, G. K. Babu, Arja Durga Prasad
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Abstract

The study aims to formulate solid lipid nanoparticles (SLNPs) of the poorly bioavailable drug α-mangostin by central composite design and evaluate their in-vitro drug characteristics. The contribution of ingredients to the physicochemical characteristics of formulated SLNPs was investigated and further utilized to optimize the final formulation. For the formulation of SLNPs, hot melt homogenization method was used followed by a ultrasonication approach. The solid lipids used in the formulation include stearic acid and Precirol ATO5; the surfactant was Poloxamer 407, and the co-surfactant was sodium taurocholate to provide the negative charge. The optimized formulation’s mean particle size, entrapment efficiency, zeta potential, and drug loading were 173.6 nm, 72.42%, −43.3 mV, and 20.46%, respectively. X-ray diffractometry confirms the amorphous nature of SLNPs. Scanning electron microscopy analysis showed spherical morphology and a particle size range between 145 and 218 nm. Differential scanning calorimetry and Fourier transform infrared studies confirmed the absence of drug-excipient interactions. According to the findings, the optimum surfactant and lipid combination produced high-quality SLNPs with stable release properties for at least 6 months at room and refrigerator temperatures. The obtained results encourage that SLNPs can be used as oral drug delivery carriers for α-Mangostin, because of their exceptional properties.
采用中心复合设计方法制备α -山竹苷固体脂质纳米颗粒
本研究旨在通过中心复合设计制备生物利用度较差的药物α-山竹苷的固体脂质纳米颗粒(SLNPs),并评价其体外药物特性。研究了各成分对所配制的SLNPs的理化特性的影响,并进一步优化了最终配方。在制备SLNPs的过程中,先采用热熔均质法,再采用超声波法。配方中使用的固体脂质包括硬脂酸和普瑞罗尔ATO5;表面活性剂为波洛沙姆407,助表面活性剂为牛磺胆酸钠提供负电荷。优化后的配方平均粒径为173.6 nm,包封效率为72.42%,zeta电位为- 43.3 mV,载药量为20.46%。x射线衍射证实了SLNPs的无定形性质。扫描电镜分析显示为球形,粒径范围在145 ~ 218 nm之间。差示扫描量热法和傅里叶变换红外研究证实没有药物-赋形剂相互作用。根据研究结果,最佳表面活性剂和脂质组合可以制备出高质量的SLNPs,在室温和冰箱温度下释放性能稳定至少6个月。结果表明,SLNPs具有独特的性质,可作为α-山竹苷的口服给药载体。
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来源期刊
journal of applied pharmaceutical science
journal of applied pharmaceutical science Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
2.20
自引率
0.00%
发文量
224
期刊介绍: Journal of Applied Pharmaceutical Science (JAPS) is a monthly, international, open access, journal dedicated to various disciplines of pharmaceutical and allied sciences. JAPS publishes manuscripts (Original research and review articles Mini-reviews, Short communication) on original work, either experimental or theoretical in the following areas; Pharmaceutics & Biopharmaceutics Novel & Targeted Drug Delivery Nanotechnology & Nanomedicine Pharmaceutical Chemistry Pharmacognosy & Ethnobotany Phytochemistry Pharmacology & Toxicology Pharmaceutical Biotechnology & Microbiology Pharmacy practice & Hospital Pharmacy Pharmacogenomics Pharmacovigilance Natural Product Research Drug Regulatory Affairs Case Study & Full clinical trials Biomaterials & Bioactive polymers Analytical Chemistry Physical Pharmacy.
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