title: Chitosan-modified PLGA polymeric nanocarriers with better delivery potential for tamoxifen.
abstract: Breast cancer is believed as the second most common cause of cancer-related deaths in women for which tamoxifen is frequently prescribed. Despite many promises, tamoxifen is associated with various challenges like low hydrophilicity, poor bioavailability and dose-dependent toxicity. Therefore, it was envisioned to develop tamoxifen- loaded chitosan-PLGA micelles for potential safe and better delivery of this promising agent. The chitosan-PLGA copolymer was synthesised and characterised by Fourier Transform-Infrared, Ultraviolet-visible and Nuclear Magnetic Resonance spectroscopic techniques. The drug-loaded nanocarrier was characterised for drug-pay load, micrometrics, surface charge and morphological attributes. The developed system was evaluated for in-vitro drug release, haemolytic profile, cellular-uptake, anticancer activity by cytotoxicity assay and dermatokinetic studies. The developed nano-system was able to substantially load the drug and control the drug release. The in-vitro cytotoxicity offered by the system was significantly enhanced vis-a-vis plain drug, and there was no substantial haemolysis. The IC50values were significantly decreased and the nanocarriers were uptaken by MCF-7 cells, noticeably. The carrier was able to locate the drug in the interiors of rat skin in considerable amounts to that of the conventional product. This approach is promising as it provides a biocompatible and effective option for better delivery of tamoxifen.
authors: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Dist. Ajmer 305 817, Rajasthan, India.
authors: Chanchal Kiran
authors: CK
authors: Thakur
authors: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Dist. Ajmer 305 817, Rajasthan, India.
authors: Nagarani
authors: N
authors: Thotakura
authors: UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles and Nanocomposites, Panjab University, 160 014 Chandigarh, India.
authors: Rajendra
authors: R
authors: Kumar
authors: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Dist. Ajmer 305 817, Rajasthan, India.
authors: Pramod
authors: P
authors: Kumar
authors: UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles and Nanocomposites, Panjab University, 160 014 Chandigarh, India; Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, 140 604 Chandigarh, India.
authors: Bhupinder
authors: B
authors: Singh
authors: Department of Pharmacy, Birla Institute of Technology and Science (BITS)-Pilani, Vidya Vihar Campus, Pilani 333031, Rajasthan, India.
authors: Deepak
authors: D
authors: Chitkara
authors: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Dist. Ajmer 305 817, Rajasthan, India. Electronic address: drkaisar@curaj.ac.in.
authors: Kaisar
authors: K
authors: Raza
mesh_terms: D000287:Administration, Topical; D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy*; D048271:Chitosan; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D005260:Female; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D061986:MCF-7 Cells; D053758:Nanoparticles / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D012869:Skin Absorption / Q000187:drug effects; D013629:Tamoxifen / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D004337:Drug Carriers; D013629:Tamoxifen; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D048271:Chitosan
keywords: Bioavailability; Cellular uptake; Confocal laser scanning microscopy; Cytotoxicity; Dermatokinetics; Nanocarriers; Nanotechnology