Abstract
Purpose: Albendazole is a poorly soluble drug which limits its oral bioavailability. The study was focussed to enhance the solubility by in-situ micronization.Methods: Albendazole microcrystals were prepared by solvent change method using gum karaya and hupu gum as stabilizing agents and the effect of each stabilizer on the prepared microcrystals were studied. FT-IR, DSC, XRD and SEM analysis were performed as a part of characterization studies. The formulations were evaluated for micromeritics, solubility and drug release. The microcrystals that had shown optimized properties were filled into suitable capsules.Results: The formulations showed reduction in particle size with uniform size distribution and three folds increase in drug release. The microcrystals had shown more than 100-folds increase in solubility compared to pure drug. Surface energy, enthalpy and crystalline nature of microcrystals were found to be reduced. Microcrystals containing gum karaya had shown more drug release. The filled-in capsules also showed increase in drug release rate. The solubility enhancement of albendazole microcrystals was mainly due to the surface adsorption of the stabilizing agents that led to reduction in surface energy and crystalline nature as substantiated by the DSC and XRD studies. The type of stabilizing agent had significant effect on dissolution rate. High affinity of albendazole with gum karaya led to faster drug release profiles.Conclusion: The study proved that in-situ micronization is an effective technique to enhance the solubility and dissolution rate of poorly soluble drugs like albendazole.
Highlights
It is well known that solubility and dissolution rate are major factors that affect bioavailability of orally administered drugs
Spray drying and super critical fluid (SCF) are found to be less reliable owing to their prolonged processing conditions and expensive equipments, whereas, in-situ micronization, a novel approach was proved to be successful in enhancement of dissolution of celecoxib, gliclazide, betamethazone, prednisolone, budesonide, itraconazole and ketoconazole.[4,5,6,7]
Gum karaya and hupu gum are hydrophilic natural polysaccharides which served as stabilizing agents in the present study
Summary
It is well known that solubility and dissolution rate are major factors that affect bioavailability of orally administered drugs. Micronization, a size reduction technique, is one of the most prominent and reliable methods to enhance drug solubility and dissolution rate In this method, the particle size distribution is kept less than 10 μm, which increases surface area-to-volume ratio, dissolution rate and adherence to surface resulting in high dissolution in GI fluids. Micronization by milling is inefficient due to high energy input that lead to disruption of the crystal lattice causing enhanced electrostatic effects, broad particle size distribution and thermodynamic instability.[1,2,3] In order to overcome above problems, various particle engineering techniques such as spray drying, super critical fluid (SCF) technologies and in-situ micronization, which facilitate production of drug in required particle size, has gained importance.
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