Process, Physicochemical Characterization and In-Vitro Assessment of Albendazole Microcrystals

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.

Incorporation of Inclusion Complexes in the Dissolvable Microneedle Ocular Patch System for the Efficiency of Fluconazole in the Therapy of Fungal Keratitis

“…Fourier transform infrared (FTIR) spectroscopy study was carried out for pure FNL, CD, physical mixture, and IC. Chemical interactions between chemical components were analyzed using the potassium bromide pellet method using the FTIR spectrophotometer (Shimadzu IR Prestige-21, Japan) at the 4000–400 cm –l wavenumber range . To create semitransparent pellets that allow light to pass through the detector, the sample and 100 mg of potassium bromide (KBr) were combined using a mortar and pounded for 5 min at 10 tons per square centimeter …”

Neusilin based liquisolid compacts of albendazole: Design, development, characterization and in vitro anthelmintic activity

“…Study In vitro dissolution study was carried out by using the USP II paddle apparatus. 900 ml 0.1N HCL was used as dissolution media, at 50 rpm and 37 ± 0.5 o C. Appropriate aliquots are withdrawn at suitable time interval (5,10,15,20,25,30,40,50, 60 min.) and filtered through whatman filter paper and diluted to 10 ml with 0.1N HCL sink conditions was maintained throughout the study.…”

“…Literature reports inclusion complex and nanoclusters of cyclodextrin, albendazoledesmotropes by supramolecularsystems with maltodextrin and glutamic acid, spray drying with lactose and other water soluble excipients, microcrystals using gum karaya and hupu gum as stabilizing agents and microcrystals with chitosan and cellulose derivatives are reported for enhancement of solubility, dissolution rate and indirectly bioavailability of albendazole [8][9][10][11][12][13][14] The low cost and broad spectrum of activity of ABZ make it typically the drug of choice for these cases. However, it's very low solubility results in low absorption through the gastrointestinal tract and in some applications, such as for the systemic diseases, high oral doses that cause adverse gastrointestinal disturbances and several detrimental side effects occur [15].…”