International Journal of Basic and Applied Chemical Sciences ISSN: 2277-2073 (Online)
An Open Access, Online International Journal Available at http://www.cibtech.org/jcs.htm
2015 Vol. 5 (3) July-September, pp.30-38/Sailaja and Anusha
Research Article
© Copyright 2014 | Centre for Info Bio Technology (CIBTech) 30
PREPARATION AND EVALUATION OF IBUPROFEN
LOADED MICROSPHERES
*Krishna Sailaja A. and Anusha K.
RBVRR Women’s College of Pharmacy, Affliated to Osmania University, Barkathpura, Hyderabad-27
*Author for Correspondence
ABSTRACT
The main objective of the present work was to prepare ibuprofen loaded ethyl cellulose microspheres by
means of solvent evaporation technique to attain the sustained release of the drug. Three formulations
were prepared (F1, F2, and F3) by altering drug to polymer ratio. The effect of polymer concentration
upon product yield, entrapment efficiency, particle size and stability was studied In vitro drug release
studies were performed and compared for the sustained release nature of the formulation. Best results
were obtained for F3 formulation with mean particle diameter of 1.4um, entrapment efficiency of 50%,
drug content of 93%. It was able to sustain the drug release up to 12hours with a drug release rate of
94.8%.
Keywords: Ibuprofen, Ethyl Cellulose, Solvent Evaporation Method, Microspheres
INTRODUCTION
The concept of advanced drug delivery has been revolutionized. The studies have been made to lend
patient derive maximum benefits of drug. The drug should be delivered to specific target sites at a rate
and concentration that permit optimal therapeutic efficacy while reducing side effects to minimum. There
are various approaches in delivering a therapeutic substance to the target site in a sustained controlled
release fashion. One such approach is using microspheres as carriers for drugs. Microspheres can be
described as small particles (in 1-1000micrometer size range) for use as carriers of drugs and other
therapeutic agents consisting of proteins or synthetic polymers which are of biodegradable in nature
(Remington, 2006; Vyaas and Khur, 2006).
Ibuprofen is a non-steroidal anti-inflammatory drug, which possess analgesic and mild antipyretic action,
because of its short half-life (1-3 hours) it was selected as model drug in this study (Saravanan et al.,
2004). Its activity is more than indomethacin, naproxen and other NSAIDS. Ibuprofen reduce the
inflammation by acting on cyclooxygenase and it inhibit the lipoxygenase pathway, which in turn
decreases the production of leukotrienes by the leukocytes and the synovial cells. It also masks T cell
suppressing the production of rheumatoid factors. Most frequent adverse effects associated with ibuprofen
are gastro intestinal disturbance; peptic ulceration and gastrointestinal bleeding. Site specific drug
delivery of ibuprofen will reduce these toxicities considerably by maintaining a low and constant level of
drug in the blood (Surendiran and Yuvaraj, 2010; Goodman and Gilmans, 2001). These sustained release
microspheres may be produced by several methods utilizing emulsion system (oil-in-water, oil-in-oil,
water-in-oil-in-water), as well as by spray drying. The common method used to produce microspheres is
emulsion solvent evaporation method. This relatively simple method enables the entrapment of a wide
range of hydrophobicdrugs (Thompson, 2007; Abbaspour et al., 2008). Ethyl cellulose is non-
biodegradable, bio-compatible, non-toxic synthetic polymer and widely used in oral and topical
formulation (Ainley and Paul, 1994). The main objective of this work was to investigate the possibility of
obtaining a sustained release formulation of ibuprofen microspheres by usingethyl cellulose in various
drug and polymer ratios.
MATERIALS AND METHODS
Ibuprofen was obtained as a gift sample from Dr. reddy Labs. Ltd, Hyderabad. Ethyl cellulose was
supplied from S.D Fine chemicals Ltd, Mumbai.
Method: preparation of ibuprofen microspheres: