Abstract. The objective of the present study was to formulate and evaluate microemulsion systems for topical delivery of clotrimazole (CTM). The solubility of CTM in various oils was determined to select the oil phase of the microemulsion systems. Pseudoternary phase diagrams were constructed to identify the area of microemulsion existence. Five CTM microemulsion formulations (M1-M5) were prepared and evaluated for their thermodynamic stability, pH, refractive index, droplet size, viscosity, and in vitro release across cellulose membrane. Among the prepared microemulsion formulations, M3 (lemon oil/ Tween 80/n-butanol/water) and M4 (isopropyl myristate/Tween 80/n-butanol/water) microemulsion systems were found to be promising according to their physical properties and CTM cumulative percentage release. Gel form of M3 and M4 were prepared using 1% Carbopol 940 as the hydrogel matrix. Both formulations were evaluated in the liquid and gel forms for drug retention in the skin in comparison to the marketed CTM topical cream and their stability examined after storage at 40°C for 6 months. Microemulsion formulations achieved significantly higher skin retention for CTM over the CTM cream. Stability studies showed that M4 preparations were more stable than M3. The in vitro antifungal activity of M4 against Candida albicans was higher than that of the conventional cream. Moreover, clinical evaluation proved the efficacy and tolerability of this preparation in the treatment of various topical fungal infections.

Objective: The objective of this research was to formulate and evaluate iron oxide nanoparticles for treatment of iron deficiency anemia (IDA). Methods:Iron oxide nanoparticles were prepared by co-precipitation method and stabilized by coating with folic acid or chitosan. The prepared nanoparticles were characterized in vitro for morphology, particle size, zeta potential, crystallinity and ultraviolet-visible (UV-Vis) absorption. In vivo studies were performed to evaluate the efficacy of the prepared nanoparticles in treating iron-deficient anemic rats compared to the commercial iron product. Results:In vitro results revealed that particle sizes were 65.95±5 nm, 220.2±12 nm and 295.3±19 nm for uncoated iron oxide nanoparticles, folic acid-coated iron oxide nanoparticles and chitosan coated iron oxide nanoparticles, respectively. UV-Vis absorption spectrum and x-ray diffraction (XRD) patterns confirmed that the prepared nanoparticles were iron oxide nanoparticles. In vivo results indicated that folic acid-coated iron oxide nanoparticles showed effective restorative action, returning haemoglobin (Hb) concentration to normal levels, where not only complete recovery of Hb within short time from the anemic state to the high normal level, but also improved Hb concentrations compared to the commercial iron product. Conclusion:The results obtained in this research work clearly indicated a promising potential of folic acid-coated iron oxide nanoparticles for the effective treatment of IDA.

The objective of this study was to evaluate the influence of solid lipid nanoparticles (SLN) loaded with the poorly water-soluble drug tamoxifen citrate (TC) on the in vitro antitumor activity and bioavailability of the drug. TC-loaded SLN were prepared by solvent injection method using glycerol monostearate (GMS) or stearic acid (SA) as lipid matrix. Poloxamer 188 or tween 80 were used as stabilizers. TC-loaded SLN (F3 and F4) prepared using GMS and stabilized by poloxamer 188 showed highest entrapment efficiency % (86.07 ± 1.74 and 90.40 ± 1.22%) and reasonable mean particle sizes (130.40 ± 9.45 and 243.80 ± 12.33 nm), respectively. The in vitro release of TC from F3 and F4 exhibited an initial burst effect followed by a sustained drug release. In vitro cytotoxicity of F3 against human breast cancer cell line MCF-7 showed comparable antitumor activity to free drug. Moreover, the results of bioavailability evaluation of TC-loaded SLN in rats compared to free TC indicated that 160.61% increase in the oral bioavailability of TC. The obtained results suggest that incorporation of the poorly water-soluble drug TC in SLN preserves the in vitro antitumor activity and significantly enhance oral bioavailability of TC in rats.

No abstract

No abstract