Abstract
Purpose: To prepare and evaluate colon specific drug delivery system of diclofenac sodium for highly localized delivery to the colon.Methods: The colon specific drug delivery system was prepared as matrix-type microspheres using Ethyl Cellulose (EC), Cellulose Acetate Phthalate (CAP), and Eudragit L 100-55 by the Solvent Evaporation Method. Microspheres were evaluated for physical properties like drug content, particle size, bulk density and angle of repose.Results: The size range of the microcapsules was 228 to 608 μm while drug content was between 74.49 and 91.50 % depending on the polymer used and the polymer ratio. Mean bulk density was < 1.2 g/ml which indicates the good flow properties, while angle of repose was < 40 o, indicating free-flowing properties. The microspheres were spherical in shape with smooth and nonporous surface, except that the microspheres containing EC and CAP exhibited a rough and porous surface. The microspheres containing Eudragit L 100-55 in combination with other polymers gave better sustained release (78.9 and 76.6 % at the end of 8 h for formulation F4 and F5, respectively) than the others.Conclusion: Microspheres prepared with drug: EC: CAP ratio of 1:2:1 show the highest drug content, possess good flow properties and surface morphology, as well as promising drug release for colon specific drug delivery of diclofenac sodium for possible treatment of colorectal cancer.Keywords: Diclofenac, Colorectal cancer, Microspheres, Ethyl cellulose, Cellulose acetate phthalate, Eudragit L 100-55
Highlights
The oral route of drug administration is the most convenient and important method of administering drugs for systemic effect due to patient acceptance and ease of administration
Dicolofenac sodium (DS) is a well-known nonsteroidal anti-inflammatory drug (NSAID). It is well absorbed in the colon, and colon specific release can be used for the treatment of various diseases like colorectal cancer and inflammatory bowel diseases [11,12,13]
To determine the mechanism of drug release and release rate kinetics of the drug from the microspheres, the in vitro drug release data was fitted to various kinetic models representing zeroorder (Q v/s t), first-order (log (Qo–Q) v/s t), Higuchi’s square root of time (Q v/s t1/2) and Korsemeyer peppas double log plot, respectively, where Q is the cumulative percentage of drug released at time t and (Qo–Q) is the cumulative percentage of drug remaining after time, t [17,18,19]
Summary
The oral route of drug administration is the most convenient and important method of administering drugs for systemic effect due to patient acceptance and ease of administration. An oral colon specific drug delivery system is intended to retard the drug release in the stomach and small intestine, but allow complete release in colon for the various diseases like colorectal cancer and inflammatory bowel diseases [1,2,3]. Dicolofenac sodium (DS) is a well-known nonsteroidal anti-inflammatory drug (NSAID) It is well absorbed in the colon, and colon specific release can be used for the treatment of various diseases like colorectal cancer and inflammatory bowel diseases [11,12,13]. As an alternative strategy of colorectal cancer treatment the colon specific delivery of NSAIDs like diclofenac is well accepted and investigated [16,17]. The present study investigates the colon specific delivery of diclofenac sodium in matrix-type microspheres prepared with ethyl celluolose, cellulose acetate phthalate and Eudragit L 100. Characterization of surface morphology where Mp and Mt are the practical mass of microspheres and theoretical mass of polymer + drug, respectively
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