Mesalazine-probiotics beads for acetic acid experimental colitis: formulation and characterization of a promising new therapeutic strategy for ulcerative colitis.
BACKGROUND
Acetic acid ulcerative colitis (UC) is an experimental condition created due to intra-rectal administration of acetic acid which causes inflammation and ulceration in the lining of colon and rectum. In such condition, the colon cannot absorb liquid from the stools, resulting in larger volume of watery stools. Mesalazine is mainly used for the treatment of UC but suffers from the drawback of having poor bioavailability. UC is also characterized by alteration in colonic microflora. The present work was focused on delivering mesalazine along with probiotic, which would facilitate to refurbish customary growth of microflora. Mesalazine and probiotic were encapsulated in pectin beads with an aim to protect the drug from gastric environment and target to colonic region.


METHODS
Pectin beads were prepared, formulation process was optimized for polymer concentration, drug concentration, cross-linking agent concentration. Formulation was characterized for surface morphology, in vitro drug release studies, determination of viable cell count, in vivo ulcer protective studies and stability studies.


RESULTS
Average particle diameter of beads was ∼1.44-1.72 mm. Drug entrapment efficiency was found to be optimal (78-79%). A sustained release of drug was observed for 5 h; nearly 60% of drug was released at the end of 10 h. Microbiological studies of probiotic showed best cell viability. In acetic acid induced UC model, Mesalazine-probiotic beads-treated group showed significant (p < 0.01) ulcer protection index with respect to free drug-treated group.


CONCLUSIONS
In conclusion, mesalazine-probiotic loaded beads may serve as a useful colon specific drug delivery system for treatment of colitis.
Pharmaceutics Research Laboratory, Shri Ram Institute of Technology-Pharmacy , Jabalpur, Madhya Pradesh , India and.
Neelam
N
Vishwakarma
Aditya
A
Ganeshpurkar
Vikas
V
Pandey
Nazneen
N
Dubey
Divya
D
Bansal
D019342:Acetic Acid / Q000633:toxicity; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D003093:Colitis, Ulcerative / Q000188:drug therapy* / Q000473:pathology; D003106:Colon / Q000378:metabolism / Q000473:pathology; D003692:Delayed-Action Preparations; D004195:Disease Models, Animal; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D065546:Drug Liberation; D008297:Male; D019804:Mesalamine / Q000008:administration & dosage* / Q000494:pharmacology; D010316:Particle Size; D010368:Pectins / Q000737:chemistry; D019936:Probiotics / Q000008:administration & dosage* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D019804:Mesalamine; D010368:Pectins; D019342:Acetic Acid
Colitis; colon targeting; mesalazine; pectin beads; probiotics