Available online at www.ijpsdr.com
77
International Journal of Pharmaceutical Sciences and Drug Research
2018; 10(2): 77-84
Research Article
ISSN: 0975-248X
CODEN (USA): IJPSPP
Entacapone – Based Floating Microspheres by Ionotropic Gelation
Technique-Morphology and Release Characteristics
Suggala Ajay
*
, Gande Suresh
Mewar University, NH-79, Gangrar, Chhitorgarh-312901, Rajasthan, India
Copyright © 2018 Suggala Ajay et al. This is an open access article distributed under the terms of the Creative Commons Attribution-
NonCommercial-ShareAlike 4.0 International License which allows others to remix, tweak, and build upon the work non-commercially, as
long as the author is credited and the new creations are licensed under the identical terms.
ABSTRACT
The main objective of the present investigation was to develop gastro retentive floating microspheres for
Entacapone. These are prepared by ionotropic gelation method with an aim of increasing the gastric residence
time and for controlled release. The polymeric mixture of Sodium alginate and HPMC K4, was used as
polymers. Sodium bicarbonate was used as the gas-forming gent. Prepared Microspheres were characterized for
the Micromeretic properties, incorporation efficiency, buoyancy test, SEM analysis, FTIR, and in vitro diffusion
studies. The diffusion studies were carried out in 0.1N HCl and the results were applied to various kinetic
models. Among the total 14 formulations F14 was optimized. The % yield of F14 formulation was found to be
98.03%. Based on optical microscopy, the particle size was 65.23 ± 0.05µm. The % buoyancy, % entrapment
efficiency and swelling index of F14 formulation was 98.16%, 97.54% and 97.67%, respectively. The cumulative
% drug release of F14 formulation was 97.99 ± 5.05% in 12 h when compared with marketed product 95.12 ± 5.01
in 1 h. SEM studies showed the particles were in spherical shape. Hence the formulated and prepared floating
Entacapone microspheres may establish to be potential candidate for safe and effective sustained drug delivery
and improve the bioavailability in the management of Parkinson’s disease.
Keywords: Entacapone, Floating microspheres, SEM, Release order kinetics.
DOI: 10.25004/IJPSDR.2018.100205 Int. J. Pharm. Sci. Drug Res. 2018; 10(2): 77-84
*Corresponding author: Mr. Suggala Ajay
Address: Mewar University, NH-79, Gangrar, Chhitorgarh-312901, Rajasthan, India
Tel.: +91-9959199492
E-mail : ajay.suggala@gmail.com
Relevant conflicts of interest/financial disclosures: The authors declare that the research was conducted in the absence of any commercial
or financial relationships that could be construed as a potential conflict of interest.
Received: 09 February, 2018; Revised: 24 February, 2018; Accepted: 26 February, 2018; Published: 25 March, 2018
INTRODUCTION
The floating drug delivery system was first described
by Davis (1968). Several approaches are currently used
to prolong gastric retention time. These include floating
drug delivery systems. FDDS are known as Hydro
dynamically balanced systems or low-density system
that has been made developed to increase the gastric
transit time of drug.
[1]
Since the last three decades
many drug molecules formulated as Gastroretentive
Drug Delivery System (GRDDS) have been patented
keeping in view its commercial success. Oral controlled
release (CR) dosage forms have been extensively used