DEVELOPMENT OF NOVEL MICROSTRUCTURED LIPID CARRIERS FOR DISSOLUTION RATE ENHANCEMENT OF ALBENDAZOLE

Objective: This study aimed to develop a microstructured lipid carrier that improves the rate of dissolution of the active pharmaceutical ingredient (API) Albendazole. Methods: A solvent diffusion method was used for the development of microstructured lipid carriers. The developed carriers were characterized by optical microscopy, infrared spectroscopy, differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and dissolution testing. Results: The morphology of the carriers was irregular, and their size tends to decrease with the addition of modifiers. Furthermore, the diffractograms and the thermograms indicated a loss of crystallinity. The thermograms and infrared spectra showed that there are not chemical incompatibilities between the API and the excipients. When the lipid carrier particles were modified with Aerosil® 200 (specifically when using this excipient at a level of 6% w/w), dissolution was increased up to 85.96±1.17 % of the drug content as per USP test for Albendazole tablets in comparison with 36.13±0.52 % for a lipid carrier formulation without modifiers. Conclusion: It was demonstrated that it is possible to develop a modified lipid carrier that improves the dissolution rate of an API with a low solubility, which was related to the amorphization of the API crystalline structure.

New Technological Approach for Glycyrrethic Acid Oral and Topical Administration

Background: 18β- glycyrrhetinic acid (Gly) is the major bioactive component of licorice roots and rhizomes of the Glycyrrhiza glabra species. It shows many activities such as antiviral, anti-inflammatory, antioxidant, antimicrobial, and antifungal, however, its use in the health field is very limited due to the low water solubility. Methods: This paper deals with the development of a new technological approach for Gly dissolution rate enhancement. It consists of Gly intercalation (guest) in the interlamellar spaces between the inorganic spaces (host) of the anionic clays “hydrotalcites” (HTlc) to obtain hybrids MgAl-HTlc-Gly and ZnAl-HTlc-Gly. Gly can find applications in both systemic and local therapies, thus advantages of the use of the hybrids in these two fields were investigated. Results: Gly dissolution rate from hybrids in the intestinal environment, site in which it is preferentially absorbed, resulted enhanced (ZnAl-HTlc-Gly > MgAl-HTlc-Gly) compared to the crystalline form, thereby, making them suitable for oral administration as dry powder in hard capsules. : For a local therapy, bioadhesive, vaginal emulgels loaded with the hybrids were developed. These showed suitable mucoadhesive property to the vaginal mucosa, necessary to prolong the residence time in the application site. The emulgel containing ZnAl-HTlc-Gly showed a faster and higher release profile than that containing MgAl- HTlc-Gly. Conclusions: The obtained results suggest that Gly intercalation into HTlc, especially in ZnAl-HTlc, allows to enhance Gly dissolution when the hybrids are formulated both as oral or topical products.