Development of Polymer based Controlled Drug Delivery Systems of Selected Antibacterial Agents

Senthilkumar, S R (2014) Development of Polymer based Controlled Drug Delivery Systems of Selected Antibacterial Agents. Doctoral thesis, The Tamilnadu Dr. M.G.R. Medical University, Chennai.


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This thesis deals with the investigations carried out by the objective of developing controlled release formulations for widely used antibiotics norfloxacin and ofloxacin for the evaluation of their controlled release potential. The first chapter of the thesis deals with a brief introduction to the conventional drug therapy, concept of sustained release drug delivery system, its relevance with respect to oral drug delivery, the anatomy and physiological considerations of the GIT, oral controlled release drug delivery system, significance and reasons for developing oral controlled release drug delivery system (CRDDS), ideal drug candidates for CRDDS, types of sustained/controlled release products, monolithic matrix system as oral CRDDS, mechanism of drug release from natural polymer matrix system and estimation of drugs in biological medium. Literature survey on the investigations that have been carried out so far on the development of controlled release drug delivery systems and current developments for the selected drug candidates is being mentioned. The aim and objectives along with the place of work is presented in the second chapter of the thesis. In particular, it explains the need for designing a suitable drug delivery system for the drug candidates selected in the present investigation. The third chapter of the thesis explains in detail the experimental procedures that were adopted, namely preformulation studies, formulation and evaluation of controlled release tablets, stability studies of the developed formulations. The fourth chapter describes in detail the experimental results obtained in the present study along with detailed discussion of the results supported by photographic plates, tables and figures. The following are some of the important findings of the present investigations; the developed matrix tablets have acceptable pharmacotechnical properties which indicate that the process can be used for the scale up studies and the drug release can be modulated significantly by varying the component of the matrix. The developed controlled release tablets of selected drug candidates have acceptable weight variation, friability and in vitro release profile. The effect of polymer concentration on the in vitro behavior was significant. In general an increase in the polymer concentration retarded the drug release significantly. The cumulative percentage drug release from the developed controlled release formulations for the optimized batches of norfloxacin and ofloxacin were 99.97 and 99.93 over a period of 12 hours respectively. The stability studies of the developed sustained release formulations of norfloxacin and ofloxacin were stable under accelerated conditions for six months. The formulated matrix tablets were capable of exhibiting sustained blood levels. The sustained and efficient drug delivery developed in the present study will maintain plasma drug levels, better, which will overcome the drawbacks associated with conventional therapy. And also, further studies involving fed state have to be carried out to establish the efficacy of the matrix tablets over conventional tablets. The pharmacokinetic parameters of the two different formulations of norfloxacin and ofloxacin were compared statistically by one way ANOVA (analysis of variance) by using SPSS version 13.0. The pharmacokinetic parameters like Cmax, Tmax, AUC0-t, t½, Kel and AUC0-∞ of the immediate release and sustained release formulations of norfloxacin and ofloxacin were found to be significantly different (p <0.05) by one way ANOVA. Based on these observations, it is concluded that the formulated matrix tablets containing Norfloxacin and Ofloxacin are capable of exhibiting sustained release properties, stable and feasible for industrial scale production. Thus they are capable of reducing the dose intake, minimize the blood level oscillations, dose related adverse effects, cost and ultimately improve the patient compliance in the therapeutic management of herpes simplex, herpes zoster for norfloxacin and nausea associated with vomiting in the radiation induced cancer therapy for ofloxacin. Further studies involving their suitability for long time application, shelf life determination, bioavailability and clinical investigations in large populations may, however, be necessary to further establish its potential and therapeutic efficacy. The formulation was optimized using response surface methodology by fitting a second-order model to the response data. The model was found to be satisfactory for describing the relationships between formulation variables and individual response variables, as well as the relationships between formulation variables and the overall desirability. The use of a desirability function appeared to be a useful approach for handling the problem of multiple responses in this case. The optimization method enabled us to predict the values of response variables and overall desirability within the experimental range with good agreement between the predicted and experimental values.

Item Type: Thesis (Doctoral)
Uncontrolled Keywords: Development of polymer, controlled drug delivery systems, antibacterial agents.
Subjects: PHARMACY > Pharmaceutics
Depositing User: Subramani R
Date Deposited: 20 Aug 2017 06:22
Last Modified: 28 Oct 2022 14:55

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