Romanian Society of Pharmaceutical Sciences

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PRE-FORMULATION, FORMULATION AND PILOT SCALE-UP STUDIES TO ESTABLISH THE QUALITATIVE AND QUANTITATIVE COMPOSITION OF AN INNOVATIVE NANOFORM DIETARY SUPPLEMENT FOR MENOPAUSAL THERAPY

SIMONA CRISAN 1,2#, ANCA LUCIA POP 1#, PAULA HENTES 2, IOANA LACATUSU 3, NICOLETA BADEA 3, CORALIA ZETU 4*, ANNE MARIE CIOBANU 1, OVIDIU NICOLAE PENES 4#, VARLAS VALENTIN 4, EMMA ADRIANA OZON 1, DENISA IOANA UDEANU 1

1Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Street, 020945, Bucharest, Romania
2R&D Centre, AC HELCOR, Victor Babes Street, 430082, Baia Mare, Romania
3Faculty of Applied Chemistry and Materials Science, The Polytechnic University of Bucharest, 1 Polizu Boulevard, 011061, Bucharest, Romania
4Faculty of Medicine, "Carol Davila" University of Medicine and Pharmacy, 37 Dionisie Lupu Street, 020021, Bucharest Romania

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The present study aimed to establish the theoretical qualitative and quantitative formula of a nanoparticle-based dietary supplement suitable for menopause therapy by integrating various herbal active ingredients – e.g. diosgenin – into a nano lipid matrix with vegetable oils. NLCs (nanostructured lipid carriers) consist of nanoparticles of standardised extracts that are present in oily form, making it challenging to incorporate them into a powder mixture. Therefore, there is a need to use modern excipients that, through their properties, absorb the oil from NLCs and convert them into powder without breaking the nanocapsules, thus providing favourable technological attributes for their processing into solid pharmaceutical forms (capsules, tablets), further allowing the active ingredients encapsulated in the nanolipid matrix, an optimal release in the body. Once the formulation of the final product had been determined, the process was scaled up to the pilot batch. The amount of dissolved diosgenin was 75.8% for tablets and 81.1% for capsules. The physico-chemical and microbiological characterization of the solid pharmaceutical forms demonstrated that the developed products containing NLCs comply with the quality requirements of the critical parameters for both pharmaceutical forms. The successful transformation of NLCs, encapsulating active plant principles, into a stable powder form to form a solid oral form represents a pivotal step in pharmaceutical technology.