ORAL CONTROL RELEASE MICROPARTICULATE DRUG DELIVERY STUDY OF ACECLOFENAC USING NATURAL POLYMER
Abstract
Objective: The present study was to prepare controlled release microsphere of aceclofenac using sodium alginate as a natural polymer.
Methods: Microspheres of the Aceclofenac sodium by ionotropic gelation technique using sodium alginate as hydrophilic carrier and three different
cross-linking agent in various proportions and different condition drying, and examines the influences of various process such as drugs polymer ratio,
different concentration of cross linkage agents, drying condition, and cross-linking time on physicochemical properties of drug loaded microbeads.
Results: Formulated drug loaded microbeads were investigated for physicochemical properties and drug release potential. All investigated properties
showed satisfactory results. While increasing in the concentration of sodium alginate, and barium chloride cross-linking time increased sphericity, size
distribution, flow properties, mean particle size, swelling ratio, and drug entrapment efficiency. No significant effect of drug polymer interactions was
observed in Fourier transform infrared studies. The drug entrapment efficiency obtained in the range of 97.59-99.88. The particle size of drug loaded
formulations was measured by an optical microscope. The mean particle size of drug-loaded microbeads was found to be in the range 948.555±1.673
to 998.41±0.428. The shape and surface characteristics were determined by scanning electron microscopy using gold sputter technique. In-vitro drug
release profile of aceclofenac sodium from microbeads was examined in simulated gastric fluid pH 1.2 for initial 2 hrs mixed phosphate buffer pH 6.8
up to 6 hrs and simulated intestinal pH 7.4 at the end of 24 hrs studies. The release of drug from the microbeads was pH dependent, showed negligible
drug release in pH 1.2. Under pH 7.4 conditions the beads will swell, and the drug release depends on the swelling and erosion process resulting the
optimum level of drug released in a sustained manner and exhibited zero-order kinetics.
Conclusion: Result of studies this system was able to prolong the drug release, minimizing the drug-related adverse effects and improve bioavailability
in different GI-tract conditions.
Keywords: Controlled drug delivery, Aceclofenac sodium, Sodium alginate, Ionotropic gelation.
Downloads
References
Lieberman HA, Lachman L, Schwartz JB. Pharmaceutical Dosage
Forms: Tablets. 2
ed., Vol. 1. USA: Marcel Dekker Inc.; 1981.
p. 285-6.
nd
Tataratil AS, Kouz J. Investigation into the mechanism of release and
formulation, development of sustained release matrix tablets of an
antiallergenic, sch-x. Int J Pharm Sci 2007;4:234-7.
Anonymous. British National Formulary. 57
ed. London: British
Medical Association and Royal Pharmaceutical Society of Great
Britain; 2009. p. 554.
th
Sastry SV, Nyshadham JR, Fix JA. Recent technological advances
in oral drug delivery - A review. Pharm Sci Technolo Today
;3:138-45.
Schwartz JB, Simonelli AP, Higuchi WI. Drug release from wax
matrices. I. Analysis of data with first-order kinetics and with the
diffusion-controlled model. J Pharm Sci 1968;57(2):274-7.
Prajapati BG, Krunal RP. Design and in vitro evaluation of novel
nicoroandil sustained release matrix tablets based on combination of
hydrophilic and hydrophobic matrix system. Int J Pharm Sci Rev Res
;1(1):33-8.
Mutalik S, Manoj K, Reddy MS, Kushtagi P, Usha AN, Anju P, et al.
Chitosan and enteric polymer based once daily sustained release tablets
of aceclofenac: In vitro and in vivo studies. AAPS PharmSciTech
;9(2):651-9.
Satyanarayana V. Preparation and evaluation of sustained release
matrix tablet of Diclofenac sodium using gum acacia and tamarind
gum. J Pharm Res 2010;3(5):156-7.
Smith AA, Muthu AK, Manavalan R. Formulation development and
evaluation of ondansetron Hydrochloride sustained release matrix
tablets. J Pharm Sci Res 2009;1(4):48-54.
Beckett AH. Alternative routes of drug administration and new drug
delivery systems. In: Breimer DD, editor. Towards Better Safety of
Drug and Pharmaceutical Products. North Hollan: Elsevier Biomedical
Press; 1980. p. 247-63.
Corveleyn S, Remon JP. Hydrochlorothiazide as a model drug. Int J
Pharm 1997;152: 215-25.
United States Pharmacopeial Convention. The United States
Pharmacopoeia, 23/National Formulary-18. Asian edition. Rock Ville,
MD: US Pharmacopoeial Convention, Inc., 2000. p. 1491-4.
Soni T, Chira N, Taja G, Pchotai N. Development of discriminating
method for dissolution of aceclofenac marketed formulation.
Dissolution Technol 2008;5:31-5.
Santanu G, Barik BB. Preparation and evaluation of aceclofenac
sustained release formulation and comparison of formulated and
marketed product. Int J Med Med Sci 2009;1(9):375-82.
World Health Organization. Indian Pharmacopoeia. 4
ed. Vol. II.
New Delhi: Controller of Publications, Government of India; 1996.
p. 730-42.
th
Gonzalez-Rodriguez ML, Holgado MA, Sánchez-Lafuente C,
Rabasco AM, Fini A. Alginate/chitosan particulate systems for sodium
diclofenac release. Int J Pharm 2002;232(1-2):225-34.
Parfitt K, editor. Martindale: The Complete Drug Reference. 32
ed.
Massachusetts: Pharmaceutical Press; 1999. p. 764-5.
Katzung BG. Basic and Clinical Pharmacology Practice. 9
ed. USA:
McGraw Hill Inc.; 38.
Brunton L, Chattner B, Knollman B. Goodman and Gillman’s The
Pharmacological Basis of Therapeutics. 10
ed., Vol. 19. New York:
Medical Publishing Division; 2001. p. 230.
Tripathi KD. Essentials of Medical Pharmacology. 5
th
ed. New Delhi:
Jaypee Brothers ; 2003. p. 199-200.
th
Ansel HC, Allen LV, Popvich JN. Pharmaceutical Dosage Forms and
Drug Delivery Systems. 7
ed. Phildelphia: Lippincott Williams and
Wilkins; 1999. p. 164-78.
Published
How to Cite
Issue
Section
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.