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Background: The current study compared the anti-arthritic efficacy of formulated Solid Lipid Nanoparticles (SLNP) of α-mangostin to its pure ethanolic extract of α-mangostin. Because of its anti-inflammatory property, Alpha-mangostin (α-mangostin) from Garcinia mangostana should be beneficial in the treatment of Rheumatoid arthritis (RA’s). Formulating a solid lipid nanoparticle with improved bioavailability will be beneficial for the efficacy of the formulation. Materials and Methods: α-mangostin and α-mangostin Solid Lipid Nanoparticle (MSLNP) were tested in a rat model at doses of 75 mg/kg and 75 mg/kg, respectively, for their effectiveness against Freund's Complete Adjuvant (FCA)-induced rheumatoid arthritis compared with the standard group (Prednisolone). On the 0th, 8th, 15th, 22nd, and 28th days, paw volumes, paw thicknesses, body weight, stair climbing test, mobility test, and arthritis score were measured. Histopathological examination of ankle joints was done after the completion of the 28th day of study. Results: MSLNP showed a significant anti-arthritic effect when compared to pure α-mangostin, possibly by lowering paw edema, paw thickness, and the arthritis score index. It also reduced hyperalgesia by improving mobility and stair climbing abilities in experimental rats. The results of histopathology confirmed the significance of MSLNP compared with α-mangostin for anti-arthritic effect. In experimental animals, the MSNLP had a better anti-rheumatoid effect compared with the pure extract. Conclusion: The observations of the present study contribute to the understanding that MSLNP has shown superior anti-arthritic activity in comparison to the pure ethanolic extract of α-mangostin. [ABSTRACT FROM AUTHOR]

The purpose of the study is to perform pre-formulation studies for alpha-mangostin (α-mangostin) and screening of additives (such as solid lipids, emulsifiers and cryoprotectants) and their combinations (ratio of lipids, ratio of drug: lipid, ratio of emulsifier: co-emulsifier and concentration of cryoprotectant) used in the formulation of solid lipid nanoparticles of α-mangostin. This screening is essential for the formulation of solid lipid nanoparticles (SLNP) that provide small particle size and PDI, high entrapment efficiency and zeta potential. This screening offers a rationale for selecting additives and their concentrations for formulating optimized SLNP. Preformulation studies showed melting point of 181.5°C, partition coefficient of 0.359 and drug solubility of 0.3072, 0.4576, 0.4892 and 0.5782 mg/mL in 1.2, 6.8, 7.0 and 7.5 pH buffers respectively. Ultimately, the DSC thermogram defines the sharp endotherm of α-mangostin at 195.98°C. Hot melt homogenization followed by ultrasonication technique is used to develop solid lipid nanoparticles. Process parameters such as homogenization speed (15,000 rpm) and ultra sonication (6 minutes) was optimized based on particle size and PDI. The optimized formulation of SLNP of α-mangostin contain 1:2:0.5:0.5:5 ratio of Drug: Solid lipid (0.8:1.2 ratio of Stearic acid: Precriol ATO5): Poloxamer 407: Sodium taurocholate: Mannitol. [ABSTRACT FROM AUTHOR]

The purpose of the present research work was to design, optimize, and evaluate fluvastatin-loaded solid lipid nanoparticles (FLV-SLNPs) using 32 factorial design for enhancing the bioavailability. Fluvastatin has several disadvantages, including the low solubility and substantial first-pass metabolism resulting in a low (30%) bioavailability and a short elimination half-life. FLV-SLNPs were prepared using the nano-emulsion technique. For the optimization of the FLV-SLNPs, a total of nine formulations were prepared by varying two independent factors at three levels, using full factorial design. In this design, lipid (A) and surfactant (B) concentrations were chosen as independent factors, whereas entrapment efficiency (Y1) and in-vitro drug release (Y2) were selected as the dependent variables. Additionally, the prepared SLNPs were characterized for X-ray diffraction, Fourier transform-infrared spectroscopy, and differential scanning calorimetry. These studies revealed that there were no interactions between the drug and the selected excipients and the selected formulation components are compatible with the drug. Pharmacokinetic studies in rats confirmed significant improvement in AUC and MRT of SLNPs in comparison with the pure drug indicating the enhanced bioavailability of SLNPs. This study provides a proof-of-concept for the fact that SLNPs can be effectively developed via experimental factorial design, which requires relatively minimal experimentation. [ABSTRACT FROM AUTHOR]