title: Development of docetaxel nanocapsules for improving in vitro cytotoxicity and cellular uptake in MCF-7 cells.
abstract: The aim of this study was to fabricate docetaxel loaded nanocapsules (DTX-NCs) with a high payload using Layer-by-Layer (LbL) technique by successive coating with alternate layers of oppositely charged polyelectrolytes. Developed nanocapsules (NCs) were characterized in terms of morphology, particle size distribution, zeta potential (ζ-potential), entrapment efficiency and in vitro release. The morphological characteristics of the NCs were assessed using transmission electron microscopy (TEM) that revealed coating of polyelectrolytes around the surface of particles. The developed NCs successfully attained a submicron particle size while the ζ-potential of optimized NCs alternated between (+) 34.64 ± 1.5 mV to (-) 33.25 ± 2.1 mV with each coating step. The non-hemolytic potential of the NCs indicated the suitability of the developed formulation for intravenous administration. A comparative study indicated that the cytotoxicity of positively charged NCs (F4) was significant higher (p < 0.05) rather than negative charged NCs (F3), plain drug (DTX) and marketed preparation (Taxotere®) when evaluated in vitro on MCF-7 cells. Furthermore, cell uptake studies evidenced a higher uptake of positive NCs (≥1.2 fold) in comparison to negative NCs. In conclusion, formulated NCs are an ideal vehicle for passive targeting of drugs to tumor cells that may result in improved efficacy and reduced toxicity of encapsulated drug moiety.
authors: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , Uttar Pradesh , India .
authors: Sandeep Kumar
authors: SK
authors: Singh
authors: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , Uttar Pradesh , India .
authors: Venkatesh Teja
authors: VT
authors: Banala
authors: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , Uttar Pradesh , India .
authors: Girish K
authors: GK
authors: Gupta
authors: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , Uttar Pradesh , India .
authors: Ashwni
authors: A
authors: Verma
authors: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , Uttar Pradesh , India .
authors: Rahul
authors: R
authors: Shukla
authors: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , Uttar Pradesh , India .
authors: Vivek K
authors: VK
authors: Pawar
authors: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , Uttar Pradesh , India .
authors: Priyanka
authors: P
authors: Tripathi
authors: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , Uttar Pradesh , India .
authors: Prabhat Ranjan
authors: PR
authors: Mishra
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D002626:Chemistry, Pharmaceutical / Q000379:methods; D000077143:Docetaxel; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems; D065546:Drug Liberation; D005260:Female; D006801:Humans; D061986:MCF-7 Cells; D046529:Microscopy, Electron, Transmission; D053769:Nanocapsules; D010316:Particle Size; D043823:Taxoids / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D053769:Nanocapsules; D043823:Taxoids; D000077143:Docetaxel
keywords: Cancer; cellular uptake; chitosan; controlled release; cytotoxicity; layer-by-layer; nanomedicine; sodium alginate