title: Biocompatible Phospholipid-Based Mixed Micelles for Tamoxifen Delivery: Promising Evidences from In - Vitro Anticancer Activity and Dermatokinetic Studies.
abstract: Tamoxifen (TAM) is frequently prescribed for the management breast cancer, but is associated with the challenges like compromised aqueous solubility and poor bioavailability to the target site. It was envisioned to develop phospholipid-based mixed micelles to explore the promises offered by the biocompatible carriers. Various compositions were prepared, employing soya lecithin, polysorbate 80, sodium chloride/dextrose, and water, by self-assembled technique. The formulations were characterized for micromeritics and evaluated for in vitro drug release, hemolysis study, dermatokinetic studies on rodents, and cytotoxicity on MCF-7 cell lines. Cellular uptake of the system was also studied using confocal laser scanning microscopy. The selected composition was of sub-micron range (28.81 ± 2.1 nm), with spherical morphology. During in-vitro studies, the mixed micelles offered controlled drug release than that of conventional gel. Cytotoxicity was significantly enhanced and IC50value was reduced that of the naïve drug. The bioavailability in epidermis and dermis skin layers was enhanced approx. fivefold and threefold, respectively. The developed nanosystem not only enhanced the efficacy of the drug but also maintained the integrity of skin, as revealed by histological studies. The developed TAM-nanocarrier possesses potential promises for safe and better delivery of TAM.
authors.affiliation: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Distt., Ajmer, Rajasthan, India, 305 817.
authors.forename: Pramod
authors.initials: P
authors.lastname: Kumar
authors.affiliation: UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles & Nanocomposites, Panjab University, Chandigarh, India, 160 014.
authors.forename: Rajendra
authors.initials: R
authors.lastname: Kumar
authors.affiliation: UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles & Nanocomposites, Panjab University, Chandigarh, India, 160 014.|Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India, 160 014.
authors.forename: Bhupinder
authors.initials: B
authors.lastname: Singh
authors.affiliation: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Distt., Ajmer, Rajasthan, India, 305 817.
authors.forename: Ruchi
authors.initials: R
authors.lastname: Malik
authors.affiliation: Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India, 160 014.
authors.forename: Gajanand
authors.initials: G
authors.lastname: Sharma
authors.affiliation: Department of Pharmacy, Birla Institute of Technology and Science, Pilani Campus, Vidya Vihar, Pilani, Rajasthan, India, 333 031.
authors.forename: Deepak
authors.initials: D
authors.lastname: Chitkara
authors.affiliation: Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India, 160 014.
authors.forename: O P
authors.initials: OP
authors.lastname: Katare
authors.affiliation: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Distt., Ajmer, Rajasthan, India, 305 817. drkaisar@curaj.ac.in.
authors.forename: Kaisar
authors.initials: K
authors.lastname: Raza
mesh_terms: D000287:Administration, Topical; D000818:Animals; D001682:Biological Availability; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D004339:Drug Compounding; D065546:Drug Liberation; D005260:Female; D006801:Humans; D061986:MCF-7 Cells; D008422:Materials Testing / Q000379:methods; D051379:Mice; D008823:Micelles; D009924:Organ Culture Techniques; D010743:Phospholipids / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption / Q000187:drug effects* / Q000502:physiology; D012995:Solubility; D013629:Tamoxifen / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008823:Micelles; D010743:Phospholipids; D013629:Tamoxifen
keywords: MCF-7 cell lines; MTT assay; bioavailability; dermal kinetics; percutaneous delivery; skin compatibility; topical delivery