Self-micro Emulsifying Drug Delivery System “SMEDDS” for Efficient Oral Delivery of Andrographolide

Q2 Pharmacology, Toxicology and Pharmaceutics Drug Delivery Letters Pub Date : 2020-02-12 DOI:10.2174/2210303109666190723145209
Sivaram Nallamolu, V. Jayanti, Mallikarjun Chitneni, L. Y. Khoon, P. Kesharwani
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引用次数: 4

Abstract

Andrographolide has potent anticancer and antimicrobial activity; however, its clinical application has been limited due to its poor water solubility as well as lack of appropriate formulation. The objective of this investigation was to formulate Self–Micro Emulsifying Drug Delivery System (SMEDDS) of andrographolide and explore its oral drug delivery aptitudes. Andrographolide SMEDDS was optimized by ternary phase approach and studied for various in vitro characteristics: Particle size, electron microscopy, polydispersity index, surface charge, dilution effect, pH stability, freeze-thaw effect, dissolution profile and stability studies. Further, antimicrobial and cytotoxic performance of andrographolide SMEDDS were evaluated in MCF–7 breast cancer cell lines and methicillin-resistant microorganisms, respectively. An optimized SMEDDS formulation of andrographolide was successfully prepared and evaluated for its drug delivery potential. The solubility of andrographolide in the developed SMEDDS formulation was increased significantly, and the drug loading was enough for making this drug clinically applicable. The andrographolide SMEDDS formulation competitively inhibited the growth of microorganisms and showed enhanced anti–microbial activity against MRSA microorganisms. The SMEDDS strategy represents one of the best approaches to deliver andrographolide via oral route, while resolving its solubility limitations.
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高效口服穿心莲内酯的自微乳化给药系统SMEDDS
穿心莲内酯具有强大的抗癌和抗菌活性;然而,由于其水溶性差以及缺乏合适的配方,其临床应用受到限制。本研究的目的是制备穿心莲内酯自微乳化给药系统(SMEDDS),并探讨其口服给药性能。采用三元相法对穿心莲内酯SMEDDS进行了优化,并对其粒径、电镜、多分散性指数、表面电荷、稀释效应、pH稳定性、冻融效应、溶出谱和稳定性等体外特性进行了研究。进一步,研究了穿心莲内酯SMEDDS在MCF-7乳腺癌细胞和耐甲氧西林微生物中的抗菌素和细胞毒性能。成功制备了穿心莲内酯的SMEDDS优化配方,并对其给药潜力进行了评价。穿心莲内酯在SMEDDS制剂中的溶解度明显提高,且载药量足够,具有临床应用价值。穿心莲内酯SMEDDS制剂竞争性抑制微生物生长,对MRSA微生物具有较强的抑菌活性。SMEDDS策略是口服给药穿心莲的最佳途径之一,同时解决了其溶解度限制。
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来源期刊
Drug Delivery Letters
Drug Delivery Letters Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.70
自引率
0.00%
发文量
30
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