Engineered polymeric nanoparticles of Efavirenz: Dissolution enhancement through particle size reduction

CORC > 昆明动物研究所 > 昆明动物研究所 > 动物模型与人类重大疾病机理重点实验室 > 分子免疫药理学

	Engineered polymeric nanoparticles of Efavirenz: Dissolution enhancement through particle size reduction
	Hari BNV[]1; Lu CL 2; Narayanan N 3; Wang RR 2; Zheng YT[]2
刊名	CHEMICAL ENGINEERING SCIENCE
	2016
卷号	155 期号:X 页码:366-375
关键词	Dissolution Size reduction Nanoparticle HIV Drug delivery
通讯作者	vedhahari@scbt.sastra.edu ; zhengyt@mail.kiz.ac.cn
合作状况	其它
英文摘要	Solubility and bioavailability of drug molecules are the key factors influencing their therapeutic effectiveness in-vivo. The desired drug concentration in systemic circulation can be achieved through the required dissolution of the drug in the biological environment which ultimately affects the pharmacological response. Efavirenz is an anti-HIV molecule with low solubility and variable bioavailability (<45%) and prescribed as first line drug with 800 mg dose. The objective of the study was to develop polymeric nanoparticles of Efavirenz and assess the dissolution enhancement, safety and efficacy using T-lymphatic cell lines infected with HIV-1(IIIB) strain. The nanoparticle formulations were developed using solvent evaporation method and characterized for its size (110-283 nm), charge (-21 to -33 mV), % entrapment efficiency (57-95%), viscosity of nanosuspension (239-4.2 cP) and surface area of the particles (1.4 m(2)/g). The fourier transform infrared analysis and differential scanning calorimetry analysis of the pure drug and nanoparticles revealed the compatibility and stability of drug in nanoparticles. The in-vitro dissolution studies of the nanoparticles in distilled water media using type-1 USP dissolution apparatus at 100 rpm showed improved drug release based on the polymer composition, as compared with marketed formulations (capsules). The cytotoxicity and therapeutic activity of nanoparticles was studied by MTT assay in C8166 cell lines and syncytium formation assay using HIV-1(IIIB) strain infected cell lines, respectively. Cell uptake of the nanoparticles was studied by confocal microscopy. The formulated nanoparticles were found to be safe and exhibiting 2-fold increase in therapeutic activity compared to pure drug, which could be attributed to improved dissolution and high cell uptake.
收录类别	SCI
资助信息	The authors are thankful to the management of SASTRA Uni- versity for financial support through Prof. TRR research scheme and providing the infrastructure facilities and Kunming Institute of Zoology, Chinese academy of Science for cell line studies where, this work was supported in part by grants from the Key Scientific and Technological Program of China (2012ZX10001-006; 2012ZX10001-007, 2012ZX09103-101-068), Yunnan Province (Y103951111), the National Natural Science Foundation of China (81102483) to Prof. Zheng.
语种	英语
内容类型	期刊论文
源URL	[http://159.226.149.26:8080/handle/152453/10638]
专题	昆明动物研究所_分子免疫药理学昆明动物研究所_动物模型与人类重大疾病机理重点实验室
作者单位	1.School of Chemical & Biotechnology, SASTRA University, Thanjavurn 613401, Tamil Nadu, India 2.Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science & Yunnan province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China 3.Department of Pharmaceutics, Jaya College of Pharmacy, Chennai 602024, Tamil Nadu, India
推荐引用方式 GB/T 7714	Hari BNV[*],Lu CL,Narayanan N,et al. Engineered polymeric nanoparticles of Efavirenz: Dissolution enhancement through particle size reduction[J]. CHEMICAL ENGINEERING SCIENCE,2016,155(X):366-375.
APA	Hari BNV[],Lu CL,Narayanan N,Wang RR,&Zheng YT[].(2016).Engineered polymeric nanoparticles of Efavirenz: Dissolution enhancement through particle size reduction.CHEMICAL ENGINEERING SCIENCE,155(X),366-375.
MLA	Hari BNV[*],et al."Engineered polymeric nanoparticles of Efavirenz: Dissolution enhancement through particle size reduction".CHEMICAL ENGINEERING SCIENCE 155.X(2016):366-375.