Abstract
The study aims to develop a microparticulate casein based delivery system by the controlled drug delivery approach using Levocetirizine dihydrochloride as the model drug. Fourier transform infrared spectroscopy (FTIR), X-ray and differential scanning calorimetry (DSC) studies substantially indicates the presence of molecularly dispersed drug within the particles with preserved stability during microencapsulation. In vitro release studies of levocetirizine dihydrochloride loaded microparticles were performed by simulating the condition of gastrointestinal tract, and showed the minimal drug leakage (less than 5%) at acidic pH (1.2) and significantly higher release at basic pH (7.4). The results were found to be critical in confirming the role of casein microparticles as potential candidate for the controlled and targeted release of levocetirizine dihydrochloride. Key words: Extended release, casein, levocetirizine dihydrochloride, steric stabilization.
Highlights
Controlled drug delivery systems are found to be vital in rectifying some of the problems associated with conventional therapy and in enhancing the therapeutic efficacy of a given drug
A total of 10 ml of casein solution in 0.1 M NaOH was prepared and the calculated amount of levocetirizine dihydrochloride was dissolved in the 10 ml of casein solution. 4 ml of this solution was dropped into a 50 ml ethylcellulose solution
Ethyl cellulose used as a steric stabilization agent plays an important role in establishing emulsion between the aqueous and organic phases, influence the formation of particles
Summary
Controlled drug delivery systems are found to be vital in rectifying some of the problems associated with conventional therapy and in enhancing the therapeutic efficacy of a given drug. The usage of microspheres as drug carriers to deliver a therapeutic agent in sustained controlled fashion has been reported (Yanhong et al, 2012). It is really fascinating to find the role of milk protein, casein, as a drug carrier mainly for the sustained delivery of various drugs (Willmott et al, 1992; Chen et al, 2006; Knepp et al, 1993; Yoav, 2010). There are mainly four casein phosphoproteins, αS1-, αS2-, β-, and κ-casein, which exist approximately in proportions of 4:1:4:1 by weight, respectively in cow milk. Their molecular weights are between 19 and 25 kDa and average isoelectric point (pI) is between 4.6 and 4.8. The usage of casein in various drug delivery studies has been well reported (Latha et al, 1994, 1995, 2000; Elzoghby et al, 2011; Arora et al, 2012)
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