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Process, Physicochemical Characterization and In-Vitro Assessment of Albendazole Microcrystals
Vandana Kr1, Prasanna Raju Yalavarthi2, Harini Chowdary Vadlamudi3
1Pharmaceutics Division, Sree Vidyanikethan College of Pharmacy, A.Rangampet, Tirupati, IN-517102.
Advanced Pharmaceutical Bulletin
|October 27, 2017
Summary
In-situ micronization effectively enhanced albendazole solubility and dissolution. Gum karaya stabilized microcrystals showed superior drug release, improving oral bioavailability for poorly soluble drugs.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Materials Science
Background:
- Albendazole exhibits poor oral bioavailability due to low solubility.
- Enhancing solubility is crucial for improving therapeutic efficacy.
Purpose of the Study:
- To enhance albendazole solubility and dissolution rate using in-situ micronization.
- To evaluate the impact of stabilizing agents (gum karaya, hupu gum) on microcrystal properties.
Main Methods:
- Albendazole microcrystals prepared via solvent change method with stabilizers.
- Characterization using FT-IR, DSC, XRD, SEM.
- Evaluation of micromeritics, solubility, and drug release.
- Capsule formulation and evaluation.
Main Results:
- Significant reduction in particle size and uniform distribution achieved.
- Over 100-fold increase in solubility and threefold increase in drug release observed.
- Reduced surface energy, enthalpy, and crystalline nature of microcrystals.
- Gum karaya yielded superior drug release compared to hupu gum.
Conclusions:
- In-situ micronization is an effective strategy for enhancing solubility and dissolution of poorly soluble drugs.
- Stabilizing agents significantly influence microcrystal properties and drug release.
- Gum karaya demonstrates high affinity for albendazole, leading to improved dissolution profiles.
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