Preparation, in vitro characterization, pharmacokinetic, and pharmacodynamic evaluation of chitosan-based plumbagin microspheres in mice bearing B16F1 melanoma.
The present study was aimed to evaluate the anti-tumor efficacy and systemic toxicity of chitosan-based plumbagin microspheres in comparison to free plumbagin. The optimized formulation had a mean particle size of 106.35 mum with an encapsulation efficiency of 80.12%. Pharmacokinetic studies showed a 22.2-fold increase in elimination half-life (t(1/2)) of plumbagin from chitosan microspheres as compared to free plumbagin. Administration of plumbagin microspheres resulted in a significant tumor growth inhibition and reduced systemic toxicity. These results suggest that chitosan-based microspheres could be a promising strategy for the systemic delivery of anti-cancer agents like plumbagin.
Mandala Rayabandla
Sunil Kumar
SK
Division of Radiobiology and Toxicology, Manipal Life Sciences Centre, Manipal, Karnataka, India.
Aithal
Kiran
K
Anandam
Aravind
A
Shavi
Gopal
G
Nayanabhirama
Udupa
U
Arumugam
Karthik
K
Musmade
Prashant
P
Bhat
Krishnamoorthy
K
Bola Sadashiva
Satish Rao
SR
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D001772:Blood Cell Count; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D048271:Chitosan; D002851:Chromatography, High Pressure Liquid; D003432:Cross-Linking Reagents; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D005976:Glutaral / Q000737:chemistry; D006207:Half-Life; D008546:Melanoma, Experimental / Q000188:drug therapy* / Q000473:pathology; D051379:Mice; D008810:Mice, Inbred C57BL; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D009285:Naphthoquinones / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D010316:Particle Size; D013056:Spectrophotometry, Ultraviolet
D000972:Antineoplastic Agents, Phytogenic; D003432:Cross-Linking Reagents; D003692:Delayed-Action Preparations; D009285:Naphthoquinones; D048271:Chitosan; D005976:Glutaral; C014758:plumbagin