Self-emulsifying System Incorporated in a Polymeric Carrier for Controlled Delivery of Thymol

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Authors

KOUTNÁ Gabriela PAVELKOVÁ Miroslava KUBOVÁ Kateřina ČUBOVÁ URBANOVÁ Martina BRUS Jiří MUSELÍK Jan VYSLOUŽIL Jakub VETCHÝ David

Year of publication 2022
Type Appeared in Conference without Proceedings
MU Faculty or unit

Faculty of Pharmacy

Citation
Description The biocompatibility and biodegradability of natural polymers make them an object of interest for many applications in biomedicine and pharmacy. Their ability to control drug release makes them very significant pharma-ceutical excipients for formulating dosage forms, especially particulate dosage forms. These advantages, together with encapsula-tion of natural active agents and the use of some soft method for their preparation, an "eco-friendly" drug dosage form could pro-vide. Many natural active ingredients today are experiencing a comeback. However, most of them have low solubility, leading to low bioavailability and ultimately low therapeutic efficacy. Therefore, a way of their modifica-tion and incorporation into the dosage form plays a crucial role in their therapeutic effec-tiveness. There are many methods to increase the bio-availability of poorly soluble drugs after oral administration. The formation of a self-emulsifying system (SES) ensures the dis-solving of lipophilic active substance and, after its reconstitution, the shape of o/w emulsion, which is necessary for drug ab-sorption either in the systemic circulation or inflamed mucosa. This systemic or local ef-fect depends on the drop size of the internal phase of the emulsion, whether the nanoemulsion, microemulsion, or macro-emulsion is created (1). Thus, this paper discusses a dosage form of pectin/alginate particles as a carrier of SES with dissolved monoterpene thymol. It is a drug with a wide range of biological effects (antimicrobial, antiviral, antifungal, anti-inflammatory, antioxidant, antineoplastic, etc.) with potential usage in nonspecific intes-tinal inflammations (NSZ). Nowadays, the treatment of NSZ includes mostly cortico-steroids and antibiotics administration, so that this new approach could become an alterna-tive to this treatment. Thymol's incorporation into the SES containing triacylglycerols, Labrasol®, and propylene glycol in ratio 2:7:1 and their subsequent solidification in pec-tin/alginate particles lead to the final solid drug form formation. The evaluation of the morphological parameters using optical and electron microscopes, evaluation of swelling capacity and dissolution profiles, and finally, the assessment of the formed emulsion after SES reconstitution in a phosphate buffer pH 6 are integral parts of this experiment.
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