Improved Oral Bioavailability, Therapeutic Efficacy, and Reduced Toxicity of Tamoxifen-Loaded Liquid Crystalline Nanoparticles

被引：22
|
作者：
Jain, Sanyog [1 ]
Heeralal, B. [1 ]
Swami, Rajan [1 ]
Swarnakar, Nitin K. [1 ]
Kushwah, Varun [1 ]
机构：
[1] NIPER, Sect 67, Dept Pharmaceut, Ctr Pharmaceut Nanotechnol, Sas Nagar Mohali 160062, Punjab, India
来源：
AAPS PHARMSCITECH | 2018年 / 19卷 / 01期
关键词：
tamoxifen; phytantriol; liquid crystalline nanoparticles; oral delivery; breast cancer; P-GLYCOPROTEIN INHIBITION; RATS POSSIBLE ROLE; MAIN METABOLITE; PHARMACOKINETICS; DELIVERY; DRUG; 4-HYDROXYTAMOXIFEN;
D O I：
10.1208/s12249-017-0851-9
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Present investigation deals with formulation and evaluation of tamoxifen (TMX)-loaded liquid crystalline nanoparticles (TMX-LCNPs) for improving oral bioavailability and safety of the existing treatment. Hexagonal Glyceryl monooleate-based TMX-LCNPs (GLCNPs) and Phytantriol-based TMX-LCNPs (PLCNPs) were prepared by dilution-through-hydrotrope method for oral administration. Oleic acid was incorporated in the lipid matrix to enhance the drug loading in the LCNPs. Optimized LCNPs displayed small particle size with a narrow distribution, sustained drug release and high gastrointestinal stability. TMX-LCNPs were found to be considerably higher cytotoxic to MCF-7 cells as compared to free TMX. Substantial fold enhancement in oral bioavailability (similar to 7- and similar to 5-folds with TMX-GLCNPs and TMX-PLCNPs, respectively) was evident followed by significant reduction in tumor burden with lesser hepatotoxicity. Out of the two LCNP formulations, PLCNPs were found to be better in convalescing the disease.
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页码：460 / 469
页数：10
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