FORMULATION AND DEVELOPMENT OF MICROSPHERES FOR THE TREATMENT OF FAMILIAL ADENOMATOUS POLYPOSIS


Md. Gulshan, M. Lakshmi Swapna Sai, T. Hemalatha, U. Jhansi Sri, N. Ramarao

Abstract


Objective: Familial adenomatous polyposis (FAP) also known as familial polyposis coli, is a hereditary disease characterized by progressive appearance of numerous polyps mainly in the large intestine. Polyps are initially benign but can easily become cancerous and as such it is a life threatening condition. Celecoxib, a cyclooxygenase-2 (COX-2) inhibitor is thought to induce cell death, and thus prevent or delay the growth of polyps. So in the present study celecoxib loaded microspheres were prepared using control release Hydroxy propyl methyl cellulose (HPMC K4M) and pH dependent polymer eudragit L 100-55 in different ratios (1:1 to 1:4) respectively. The main objective of the study is to identify the polymer concentration required to prevent the drug release in stomach region and promotes in intestinal region.

Methods: Emulsification solvent evaporation method was selected for the preparation and all the optimized formulations were evaluated for drug-polymer interactions, percentage yield, micrometric properties, entrapment efficiency, particle size analysis, differential scanning calorimetry and in vitro dissolution study.

Results: Drug and polymer interactions were evaluated by using FTIR and DSC. The FTIR spectrum and DSC thermograms stated that drug and polymer are compatible to each other. The micrometric properties of drug loaded microspheres were carried out and they were found to be as the angle of repose (18.26 °-40.69 °), bulk density (0.2846-0.3875), tapped density (0.4111-0.5428), Carr’s index (9.66-14.77), Hausner’s ratio (1.112-1.2642) which were within the limits. In vitro dissolution, drug release was found to be from 4.5 to 6.5 h for the prepared four formulations (F1–F4). From the kinetic data modeling the order of drug release was found to be zero order and korsmeyer-peppas with n value above 0.5 for all the formulations indicating non-fickian diffusion.

Conclusion: All the result demonstrated that celecoxib microspheres can be effectively used in the treatment of familial adenomatous polyposis


Keywords


Microspheres, Polyposis, Eudragit, pH dependent

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References


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About this article

Title

FORMULATION AND DEVELOPMENT OF MICROSPHERES FOR THE TREATMENT OF FAMILIAL ADENOMATOUS POLYPOSIS

Keywords

Microspheres, Polyposis, Eudragit, pH dependent

DOI

10.22159/ijap.2017v9i5.19731

Date

15-09-2017

Additional Links

Manuscript Submission

Journal

International Journal of Applied Pharmaceutics
Vol 9, Issue 5 (Aug-Sep), 2017 Page: 66-72

Online ISSN

0975-7058

Statistics

48 Views | 22 Downloads

Authors & Affiliations

Md. Gulshan
Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh, India-522034
India

M. Lakshmi Swapna Sai
Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh, India-522034
India

T. Hemalatha
Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh, India-522034
India

U. Jhansi Sri
Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh, India-522034
India

N. Ramarao
Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh, India-522034
India


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