Pre-Formulation, Formulation and Pilot Scale-Up Studies to Establish the Qualitative and Quantitative Composition of an Innovative Nanoform Dietary Supplement for Menopausal Therapy

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.

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Excipients used in the formulation of oral solid form (tablets/capsules):

Sorbitol (NEOSORB P 60W, Roquette); Silica colloidal anhydrous (HDK N20 – Pyrogenic Silica, Wacker); Hydroxypropyl cellulose (KLUCEL, Ashland); Mannitol (PEARLITOL 160C, Roquette); Magnesium Stearate (Magnesium Stearate EP, Mosselman); Calcium Carbonate (Calcium Carbonate, AIS & A Prodimpex); Calcium Phosphate Anhydrous (DI-CAFOS A60, Budenheim); Microcrystalline Cellulose 102 (ACECEL 102, Sigachi Industries Limited); Magnesium Aluminometasilicate (NEUSILIN UFL2, Fuji Chem. Ind.); Spray-dried granular amorphous Silica (FUJISIL, Fuji Chemical Industries).

SIMONA CRISAN, ANCA LUCIA POP, PAULA HENTES, IOANA LACATUSU, NICOLETA BADEA, CORALIA ZETU, ANNE MARIE CIOBANU, OVIDIU NICOLAE, PENES, VARLAS VALENTIN, EMMA ADRIANA OZON, DENISA IOANA UDEANU, Pre-Formulation, Formulation and Pilot Scale-Up Studies to Establish the Qualitative and Quantitative Composition of an Innovative Nanoform Dietary Supplement for Menopausal Therapy, FARMACIA, 2024, Vol. 72, 2, Manuscript received: January 2024