Pectin/Kollicoat SR30D isolated films for colonic delivery [I]: a comparison of normal and colitis-induced models to assess the efficiency of microbially triggered drug delivery.
OBJECTIVE
The purpose of the study was to evaluate digestion of pectin/Kollicoat SR30D free films for colonic delivery in vitro and in vivo.


METHODS
Free films containing different ratios of pectin to Kollicoat SR30D were prepared by casting/solvent evaporation method. An in-vitro comparison of swelling, degradation and permeability of the free films was carried out in simulated colon fluids containing caecal contents from normal rats with colitis induced by 2,4,6-trinitrobenzene sulfonic acid (TNBS) or oxazolone. A comparative in-vivo evaluation of degradation was also conducted in normal and colitis-induced model rats.


RESULTS
The pectin within the mixed films was susceptible to rat colonic bacterial enzymes. The extent of digestion correlated with the amount of pectin present within the film. In vitro, the swelling index, drug permeability and extent of film digestion in simulated colon fluids with caecal contents obtained from normal rats were higher than from TNBS- or oxazolone-induced model rats, whereas in-vivo degradation was similar in the three groups of rats. The pectin/Kollicoat SR30D free films were completely degraded in the colitis-induced rats.


CONCLUSIONS
Pectic/Kollicoat SR30D films may be useful as coatings to target delivery of drugs to the colon.
Wei
He
H
Department of Pharmaceutics, School of Pharmaceutical Science, Hebei Medical University, ShiJiaZhuang, PR China. hhewwei@126.com
Li-Fang
Fan
F
Yong-Zhen
Chang
C
Bai
Xiang
X
Qing
Du
D
Min
Bai
B
Feng
Wang
W
Min
Qing
Q
De-Ying
Cao
C
D000818:Animals; D002432:Cecum / Q000187:drug effects / Q000382:microbiology / Q000503:physiopathology; D003092:Colitis / Q000139:chemically induced / Q000503:physiopathology*; D003106:Colon / Q000187:drug effects* / Q000201:enzymology / Q000382:microbiology*; D004195:Disease Models, Animal; D016503:Drug Delivery Systems / Q000379:methods*; D005472:Fluorouracil / Q000592:standards / Q000633:toxicity; D005898:Glass / Q000737:chemistry; D010081:Oxazolone / Q000633:toxicity; D010368:Pectins / Q000737:chemistry* / Q000494:pharmacology; D010539:Permeability; D011145:Polyvinyls / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D013227:Steam; D013696:Temperature; D014302:Trinitrobenzenesulfonic Acid / Q000633:toxicity
D011145:Polyvinyls; D013227:Steam; D010081:Oxazolone; C013215:polyvinyl acetate; D010368:Pectins; D014302:Trinitrobenzenesulfonic Acid; D005472:Fluorouracil