Curcumin loaded pH-sensitive nanoparticles for the treatment of colon cancer.
The investigation was aimed at designing pH-sensitive, polymeric nanoparticles of curcumin, a natural anti-cancer agent, for the treatment of colon cancer. The objective was to enhance the bioavailability of curcumin, simultaneously reducing the required dose through selective targeting to colon. Eudragit S100 was chosen to aid targeting since the polymer dissolves at colonic pH to result in selective colonic release of the entrapped drug. Solvent emulsion-evaporation technique was employed to formulate the nanoparticles. Various process parameters were optimized and the optimized formulation was evaluated for particle size distribution and encapsulation efficiency before subjecting to freeze-drying. The freeze dried product was characterized for particle size, drug content, DSC studies, particle morphology. Anti-cancer potential of the formulation was demonstrated by MTT assay in HT-29 cell line. Nanometric, homogeneous, spherical particles were obtained with encapsulation efficiency of 72%. Freeze-dried nanoparticles exhibited a negative surface charge, drug content of > 99% and presence of drug in amorphous form which may result in possible enhanced absorption. MTT assay demonstrated almost double inhibition of the cancerous cells by nanoparticles, as compared to curcumin alone, at the concentrations tested. Enhanced action may be attributed to size influenced improved cellular uptake, and may result in reduction of overall dose requirement. Results indicate the potential for in vivo studies to establish the clinical application of the formulation.
Prajakta
Dandekar
D
Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, N.P Marg, Matunga, Mumbai 400019, India.
Ratnesh
Jain
J
Chandan
Kumar
K
Suresh
Subramanian
S
Grace
Samuel
S
Meera
Venkatesh
V
Vandana
Patravale
P
D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry; D002470:Cell Survival / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D003460:Crystallization / Q000379:methods; D003474:Curcumin / Q000008:administration & dosage* / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D019073:HT29 Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008422:Materials Testing; D008968:Molecular Conformation; D053769:Nanocapsules / Q000008:administration & dosage* / Q000737:chemistry*; D050997:Nanomedicine / Q000379:methods*; D010316:Particle Size; D011109:Polymethacrylic Acids / Q000737:chemistry*; D013499:Surface Properties; D016896:Treatment Outcome
D000970:Antineoplastic Agents; D053769:Nanocapsules; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D003474:Curcumin