ABSTRACT
@#Introduction: Amlodipine besylate is a calcium channel blocker indicated for hypertension and angina. It is described as slightly soluble in water and due to its limited solubility, it may result in poor bioavailability. The aim of this study is to enhance the solubility of amlodipine besylate using solvent evaporation method and microemulsion technique and to compare the two methods. Method: Solid dispersions (SD) of amlodipine besylate were developed by employing solvent evaporation method. PEG6000 was the polymer of choice and different drug:polymer ratios were used. Evaluation of the prepared SDs include solubility studies, dissolution studies and scanning electron microscopy (SEM). As for the microemulsion technique, microemulsions were prepared by phase titration method and the optimized microemulsion formulation was then characterized for solubility studies and dissolution studies. Results: SD3 with drug:polymer ratio of 1:4 achieved the highest solubility which was 96.97 mg/ml ± 0.92 whereas the solubility of the optimized microemulsion was found to be 112.54 mg/ml ± 0.92. In solvent evaporation method, as the drug:polymer ratio increases, the solubility and dissolution rate of SDs increases. Conclusion: The two methods had significantly enhance the solubility of amlodipine besylate however the microemulsion technique showed better solubility profile.
ABSTRACT
Objective To assess the immunopotentiality of Ayurvedic polyherbal preparations, “Saribadi” and “Anantamul Salsa”. Methods Freshly prepared BALB/c mice splenocytes were cultured with “Saribadi” or “Anantamul Salsa” treatment [doses of 0.25%, 0.50%, 0.75%, 1.00%, 1.50%, 2.00%, 3.00% and 4.00% (v/v)] at 37 °C for 5 days. The immunoglobulin M (IgM) production and lymphocytes proliferation were determined by ELISA and MTT methods, respectively. Endotoxin contamination was assessed by treating the preparations with polymyxin B. Results The doses of “Saribadi” [0.25%, 0.50%, 0.75% and 1.00% (v/v)] significantly increased IgM productions (0.966, 0.728, 0.695 and 0.615 μg/mL vs. control 0.265 μg/mL) and lymphocytes proliferation [absorbance 0.311, 0.394, 0.372 and 0.334 optical density (OD) vs. control 0.162 OD]. Similarly, the doses of “Anantamul Salsa” [0.50%, 0.75%, 1.00% and 1.50% (v/v)] promoted IgM productions (0.933, 0.919, 0.917 and 0.892 μg/mL vs. control 0.502 μg/mL) and the doses of “Anantamul Salsa” [0.50%, 0.75%, 1.00%, 1.50%, 2.00%, and 3.00% (v/v)] stimulated lymphocytes proliferation (absorbance 0.395, 0.326, 0.440, 0.398, 0.452 and 0.355 OD vs. control 0.199 OD). The activity of “Saribadi” and “Anantamul Salsa” was not retarded by the treatment of preparations with polymyxin B. Conclusions Immunomodulatory activity of “Saribadi” and “Anantamul Salsa” was unveiled for the first time. “Saribadi” and “Anantamul Salsa” possess immunostimulating potential acting through the induction of lymphocyte proliferation and IgM production. These preparations may be useful in strengthening immune responses. However, further cellular and in vivo studies are required.