Development of plumbagin-loaded phospholipid-Tween® 80 mixed micelles: formulation, optimization, effect on breast cancer cells and human blood/serum compatibility testing

• Published in: Therapeutic delivery Vol. 4; no. 10; p. 1247
• Main Authors: Bothiraja, Chellampillai, Kapare, Harshad S, Pawar, Atmaram P, Shaikh, Karimunnisa S
• Format: Journal Article
• Language: English
• Published: England 01.10.2013
• Subjects: Antineoplastic Agents, Phytogenic - administration & dosage; Antineoplastic Agents, Phytogenic - chemistry; Antineoplastic Agents, Phytogenic - metabolism; Antineoplastic Agents, Phytogenic - pharmacology; Antineoplastic Agents, Phytogenic - toxicity; Blood Proteins - metabolism; Breast Neoplasms - pathology; Cell Survival - drug effects; Chemistry, Pharmaceutical; Delayed-Action Preparations; Drug Carriers; Drug Stability; Female; Hemolysis - drug effects; Humans; Kinetics; MCF-7 Cells; Micelles; Nanoparticles; Nanotechnology; Naphthoquinones - administration & dosage; Naphthoquinones - chemistry; Naphthoquinones - metabolism; Naphthoquinones - pharmacology; Naphthoquinones - toxicity; Particle Size; Phospholipids - chemistry; Phospholipids - metabolism; Phospholipids - toxicity; Polysorbates - chemistry; Polysorbates - metabolism; Polysorbates - toxicity; Protein Binding; Solubility; Technology, Pharmaceutical - methods
• ISSN: 2041-5990
• DOI: 10.4155/TDE.13.92

Phospholipid and Tween(®) 80 mixed micelles were investigated as injectable nanocarriers for the natural anticancer compound, plumbagin (PBG), with the aim to improve anticancer efficiency. PBG-loaded mixed micelles were fabricated by self-assembly; composition being optimized using 3(2) factorial design. Optimized mixed micelles were spherical and 46 nm in size. Zeta potential, drug loading and encapsulation efficiency were 5.04 mV, 91.21 and 98.38% respectively. Micelles demonstrated sustained release of PBG. Micelles caused a 2.1-fold enhancement in vitro antitumor activity of PBG towards MCF-7 cells. Micelles proved safe for intravenous injection as PBG was stable at high pH; micelle size and encapsulation efficiency were retained upon dilution. Developed mixed micelles proved potential nanocarriers for PBG in cancer chemotherapy.