Authors: Bhatt Kruti Nileshbhai1, Dr. Jitendra Patel2, Dr. U.M. Upadhyay
Abstract: Multiparticulate drug delivery system is increasing desire effect over single unit dosages forms because of their potential benefits. Multiparticulate systems provide predictable gastric emptying, no risk of dose dumping, flexible release pattern and increased bioavailability with less inter and Intra subject variability. The aim of this review is to provide the main multiparticulate pulsatile delivery system, for which the swelling and rupturing and changed permeability of the coating membrane is primarily involved in the control of release. Ulcerative colitis is the chronic relapsing multifactorial gastrointestinal inflammatory bowel disease, which is characterized by bloody diarrhea, bowel dysfunction, anaemia. The main aim is to overcome ulcerative colitis is appropriate local targeting and drug-related side-effects. To overcome these problems, microparticulate systems seems to be a promising approach for controlled and sustained drug release after oral administration, with this drug delivery system increasing immense importance for the local targeting drug to the colon at a controlled and sustained rate. Prior to the development of any system, due consideration must be given to the physiological changes that occur in the disease state that might affect the performance of such a system. In spite of such physiological constraints to drug delivery to the colon, several colon-targeted formulations have been successfully commercialized in US and European markets. Few of the commercialized products are listed in Table 1. Several reviews have been published reporting the research that has gone into the development of perorally delivered single unit colon targeted drug delivery systems (24-30). In general, four primary approaches have been proposed for colon targeted delivery, namely prodrugs, pH-dependent system, time-dependent systems and colonic microflora activated systems (27). A brief summary of some of the colon targeted formulations based on the above mentioned conventional approaches is given in Table 2. Single unit colon targeted drug delivery system may suffer from the disadvantage of unintentional disintegration of the formulation due to manufacturing deficiency or unusual gastric physiology that may lead to drastically compromised systemic drug bioavailability or loss of local therapeutic action in the colon. Recently, much emphasis is being laid on the development of multiparticulate dosage forms in comparison to single-unit systems because of their potential benefits like increased bioavailability, reduced risk of systemic toxicity, reduced risk of local irritation and predictable gastric emptying (31). Multiparticulate approaches tried for colonic delivery include includes formulations in the form of pellets, granules, microparticles and nanoparticles. The use of multiparticulate drug delivery systems in preference to single unit dosage forms for colon targeting purposes dates back to 1985 when Hardy and co-workers (32) showed that multiparticulate systems enabled the drug to reach the colon quickly and were retained in the ascending colon for a relatively long period of time. Because of their smaller particle size as compared to single unit dosage forms, these systems are capable of passing through the GI tract easily, leading to less inter-and intra-subject variability. Moreover, multiparticulate systems tend to be more uniformly dispersed in the GI tract and also ensure more uniform drug absorption (33-35).
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