OBJECTIVE: This research was proposed to develop a co-processed excipient composed of xylitol, mannitol, and microcrystalline cellulose for the formulation of ODTs.
METHODS: A total of 11 formulations of co-processed excipients with different ratios of ingredients were prepared, which were then compressed into ODTs, and their characteristics were thoroughly examined. The primary focus was on evaluating the disintegration time and hardness of the tablets, as these factors are important in ensuring the ODTs meet the desired criteria. The model drug, Mirtazapine was then incorporated into the chosen optimized formulation.
RESULTS: The results showed that the formulation comprised of 10% xylitol, 10% mannitol and 80% microcrystalline cellulose demonstrated the fastest disintegration time (1.77 ± 0.119 min) and sufficient hardness (3.521 ± 0.143 kg) compared to the other formulations. Furthermore, the drug was uniformly distributed within the tablets and fully released within 15 min.
CONCLUSION: Therefore, the developed co-processed excipients show great potential in enhancing the functionalities of ODTs, offering a promising solution to improve the overall performance and usability of ODTs in various therapeutic applications.
METHODS: The titration method was used to prepare LPV-loaded SNEDDS (LPV-SNEDDS). Six different pseudo-ternary phase diagrams were constructed to identify the nanoemulsifying region. The developed formulations were chosen in terms of globule size < 100 nm, dispersity ≤ 0.5, dispersibility (Grade A) and% transmittance > 85. Heating-cooling cycle, freeze-thaw cycle, and centrifugation studies were performed to confirm the stability of the developed SNEDDS.
RESULTS: The final LPV-SNEDDS (L-14) droplet size was 58.18 ± 0.62 nm, with polydispersity index, zeta potential, and entrapment efficiency (EE%) values of 0.326 ± 0.005, -22.08 ± 1.2 mV, and 98.93 ± 1.18%, respectively. According to high-resolution transmission electron microscopy (HRTEM) analysis, the droplets in the optimised formulation were < 60 nm in size. The selected SNEDDS released nearly 99% of the LPV within 30 min, which was significantly (p < 0.05) higher than the LPV-suspension in methylcellulose (0.5% w/v). It indicates the potential use of SNEDDS to enhance the solubility of LPV, which eventually could help improve the oral bioavailability of LPV. The Caco-2 cellular uptake study showed a significantly (p < 0.05) higher LPV uptake from the SNEEDS (LPV-SNEDDS-L-14) than the free LPV (LPV-suspension).
CONCLUSION: The LPV-SNEDDS could be a potential carrier for LPV oral delivery.
METHODS: The liquids were adsorbed on microcrystalline cellulose, and all developed formulations were compressed using 10.5 mm shallow concave round punches.
RESULTS: The resulting tablets were evaluated for different quality-control parameters at pre- and postcompression levels. Simvastatin showed better solubility in a mixture of oils and Tween 60 (10:1). All the developed formulations showed lower self-emulsification time (˂200 seconds) and higher cloud point (˃60°C). They were free of physical defects and had drug content within the acceptable range (98.5%-101%). The crushing strength of all formulations was in the range of 58-96 N, and the results of the friability test were within the range of USP (≤1). Disintegration time was within the official limits (NMT 15 min), and complete drug release was achieved within 30 min.
CONCLUSION: Using commonly available excipients and machinery, SEDDS-based tablets with better dissolution profile and bioavailability can be prepared by direct compression. These S-SEDDSs could be a better alternative to conventional tablets of simvastatin.
METHODS: Mangosteen peel extract was formulated into amorphous solid dispersions using polyvinylpyrrolidone K30 at a 1:3 polymer ratio via solvent evaporation and fluidized bed drying methods. Solubility enhancement was evaluated under standardized conditions, and α-glucosidase inhibitory activity was assessed through IC50 determination. Comparative analysis against acarbose and quercetin standards was performed.
RESULTS: Solvent evaporation achieved 2.1-fold solubility enhancement, while fluidized bed drying yielded 1.8-fold improvement. The mangosteen peel extract demonstrated superior α-glucosidase inhibition (IC50 = 20.13 ± 0.02 μg/mL) compared to acarbose (IC50 = 379.75 ± 0.57 μg/mL) but remained less potent than quercetin (IC50 = 2.97 ± 0.05 μg/mL). When normalized to equivalent α- mangostin concentrations, fluidized bed drying preserved inhibitory activity more effectively (IC50 = 112.87 ± 0.06 μg/mL) than solvent evaporation (IC50 = 1238.48 ± 0.51 μg/mL).
DISCUSSION: The manufacturing method significantly influenced both solubility and biological activity. Solvent evaporation maximized solubility enhancement but compromised enzyme inhibitory potency, whereas fluidized bed drying maintained superior inhibitory activity despite moderate solubility improvement. This trade-off suggests that formulation strategy selection should prioritize the desired therapeutic outcome.
CONCLUSION: Amorphous solid dispersion successfully enhanced both solubility and α-glucosidase inhibitory activity of mangosteen peel extract. Fluidized bed drying represents the optimal manufacturing approach for preserving enzyme inhibition while achieving meaningful solubility enhancement, positioning α-mangostin as a promising candidate for natural antidiabetic drug development.