Design and In-Vitro Characterization of Metadoxine Buccal Patches using Borassus Flabellifer Fruit Resin - A Novel Mucoadhesive Polymer

Hariharshan, V (2017) Design and In-Vitro Characterization of Metadoxine Buccal Patches using Borassus Flabellifer Fruit Resin - A Novel Mucoadhesive Polymer. Masters thesis, Sri Ramakrishna Institute of Paramedical Sciences, Coimbatore.


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INTRODUCTION: Tablets have always been the most preferred formulation for drug administration via oral route. Tablets constitute around 70-80% of the total formulations available in the market. However, there are limitations which make tablets as a secondary option when formulating new drugs. This is attributed to the physicochemical properties as well as pharmacokinetic parameters of the drug intended for formulation such as aqueous solubility, bioavailability, absorption rate and half-life etc. Such limitations can be overcome by opting alternate routes of drug administration. One such route is buccal drug delivery. OBJECTIVES OF THE STUDY: a) To establish the mucoadhesive property of a natural polymer obtained from fruits of B. flabellifer (Palmyra palm) plant. b) To determine whether this novel natural polymer possess sustained release or immediate release pattern. c) To formulate the drug Metadoxine in a novel dosage form, which is currently unavailable in the market. d) To propose a new theory for calculation of dose, by incorporating thickness factor. e) To determine whether the change in dosage form can enhance the bioavailability and thereby reduce the dosing frequency as well as dose dumping of the particular drug. SUMMARY: Natural polymers are trending as a reliable alternative for synthetic and semi synthetic polymers, in the development of a large number of novel drug delivery systems. One such new alternative to be used as a mucoadhesive polymer- B. flabellifer Fruit resin, especially for buccal drug delivery was introduced. The novel polymer, in combination with two other natural polymers (Pectin & Sodium alginate) and one synthetic polymer (PVA), was used to formulate a buccal drug delivery system containing Metadoxine. This drug was chosen due to its low half-life (maximum of 60 min) and attempt was made to reduce its dose by sustaining its release. Also alcoholism is a serious social and health issue affecting a significant amount of world population and hence a therapeutic alternative to cure alcoholism is a need of the hour. Compatibility studies carried out with the help of FT-IR spectrometer indicated that there are no chemical interactions between the drug and the polymers used, including BFR. The calibration graph of Metadoxine was obtained by a validated UV spectrophotometric method at λmax of 324 nm. BFR was extracted from ripened palm fruit; stored and used for formulating 9 formulations in the ratios BFR : Pectin - 3:5, 4:4, 5:3 / BFR : SA – 4:2, 4:3, 4:4 and BFR : PVA - 3:5, 4:4, 5:3 respectively (the numbers in the ratios indicate the polymer concentration in percentage). A backing membrane of 4% PVA was also coated over one side of all formulations. Physico-chemical properties such as thickness, weight variation, folding endurance, swelling index, surface pH, drug content and bioadhesion strength were evaluated appropriately and, the results were tabulated and compared. In-vitro diffusion study was also performed to examine the release pattern of the formulations, which was extended to determine the kinetics and mechanism of the release. CONCLUSION: Metadoxine buccal patches were formulated and evaluated successfully by solvent casting method; following standard operating procedures. The evaluation tests revealed that B. flabellifer is a suitable polymer for developing a sustained release buccal drug delivery system. Among the developed buccal patches, the formulation F7 with a polymer combination of 3% w/v BFR and 5% w/v PVA seems to be an optimized formulation, since it exhibits better folding endurance, uniformity of drug content, and sustained release of drug. Therefore, Metadoxine which exhibits lower elimination halflife can be incorporated in buccal drug delivery systems, in order decrease the dose frequency and thereby decreasing the possibility of dose dumping. It also should be noted that, concentration of BFR is directly proportional to the bioadhesion strength and hence BFR justifies its selection as a novel mucoadhesive polymer of natural origin.

Item Type: Thesis (Masters)
Additional Information: REG.No: 261510151
Uncontrolled Keywords: Design ; In-Vitro Characterization ; Metadoxine Buccal Patches ; Borassus Flabellifer Fruit Resin ; A Novel Mucoadhesive Polymer
Subjects: PHARMACY > Pharmaceutics
Depositing User: Ravindran C
Date Deposited: 23 Mar 2018 06:38
Last Modified: 23 Mar 2018 06:38

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