Objective of the present investigation was enthused by the possibility to develop solid lipid nanoparticles (SLNs) of hydrophilic drug acyclovir. Also study vitro and vivo drug delivery. Methods: Drug loaded SLNs (ACV-SLNs) were prepared by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state with formula optimization study (Different lipid concentration, drug loaded, homogenization / stirring speed and compritol 888ATO: drug ratio). ACV - SLN incorporated in cream base. The pH was evaluated and rheological study. Drug release was evaluated and compared with simple cream- drug, ACV – SLN with compritol 888ATO and marketed cream. The potential of SLN as the carrier for dermal delivery was studied. Results: Particle size analysis of SLNs prove small, smooth, spherical shape particle ranged from 150 to 200 nm for unloaded and from 330 to 444 nm for ACV loaded particles. The EE% for optimal formula is 72% with suitable pH for skin application. Rheological behavior is shear thinning and thixotropic. Release study proved controlled drug release for SLNs especially in formula containing compritol88 ATO. Stability study emphasized an insignificant change in SLNs properties over 6 month. In-vivo study showed significantly higher accumulation of ACV in stratum corneum, dermal layer, and receptor compartment compared with blank skin. Conclusion: AVC-loaded SLNs might be beneficial in controlling drug release, stable and improving dermal delivery of antiviral agent(s).
Combining drugs with different mechanism of action in nanocarriers is becoming a promising strategy in cancer therapy. In the present study, the anticancer activity of the combination of doxorubicin (DOX) and pravastatin (PRV) loaded in nanoemulsions (NEs) was evaluated in HCT 116 colon cancer cells. The NE formulas (NEa and NEb) consisted of different weight fractions of the surfactant mixture of Eumulgin HRE 40/ Soya phosphatidylcholine/ sodium oleate at a fixed weight ratio of 3.5:3.0:3.5, cholesterol (CHO), Tris- HCl buffer (pH 7.22), and 1-octanol. The cytotoxicity of the drug formulas, loaded in either water or NEs, was assessed through 3-(4, 5 Dimethylthiazole- 2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assay, while the mechanism of cell death was determined by observing the morphological changes of treated cells under light microscope and identifying apoptosis by using the ApopNexin FITC kit and DAPI nuclear staining. It has been found that reducing the concentration of DOX from 15 to 7.5µM by formulating it with 7.5µM of PRV in NEa (NEa (1 DOX:1 PRV)) has preserved its cytotoxicity against HCT-116 cancer cells. The present study proved that the combination of the PRV and DOX loaded in NEa formulations improved the therapeutic potential of both of PRV and DOX as anticancer drugs.
This study was aimed to determine the characteristic and tretinoin release in nanoemulsion using virgin coconut oil (VCO) as oil phase compared with emulsion. The characteristics of the tretinoin nanoemulsion (TN) were observed in terms of droplet morphology by Transmission Electron Microscopy (TEM) and droplet size by particle analyzer and light microscope and the pH value by pH meter. The release rate of tretinoin in nanoemulsion and emulsion was measured by Franz diffusion cell using cellophane membrane. Result of this research showed the droplet morphology of tretinoin nanoemulsion and emulsion were spherical. The droplet size of tretinoin nanoemulsion (72.57 ± 18.16 nm) was smaller than tretinoin emulsion (10.54 ± 0.61 m). The pH value of tretinoin nanoemulsion and tretinoin emulsion was 6.24 ± 0.01 and 6.21 ± 0.02. In interval times 5 – 60 minutes the tretinoin release rate (flux) in nanoemulsion was 0.158 ± 0.016 µg/cm2 /minute higher than in emulsion which was 0.048 ± 0.016 g/cm2 /minute. In interval times 60 – 180 minutes, tretinoin release rate (flux) in nanoemulsion was 0.046 ± 0.005 g/cm2 /minute lower than in emulsion which was 0.090 ± 0.016 g/cm2 /minute. In interval times 180 – 720 minutes the tretinoin release rate (flux) in nanoemulsion was 0.025 ± 0.001 g/cm2 /minute which had no significant different compared to in emulsion which was 0.022 ± 0.002 g/cm2 /minute. The statistical analysis of the tretinoin release rate value using independent T-test result was known that there were significant different between nanoemulsion (TN) and emulsion (TE). Conclusion: The droplet size of tretinoin nanoemulsion was below 100 nm, pH value 6.24 ± 0.01 and the tretinoin release rate in nanoemulsion using VCO was higher than in emulsion
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