ABSTRACT
Objective: The aim of present study was to prepare nanostructured lipid carriers (NLCs) based Triamcinolone acetonide (TA). Methods: Nanostructured lipid carriers (NLCs) consisted of solid lipid and liquid lipid are a new type of lipid nanoparticles, prepared by using solvent diffusion and high pressure homogenization methods, which offer the advantage of improved drug loading capacity and release properties. Glyceryl monostearate selected as the solid lipid, capmul MCM C8 as the liquid lipid, polyvinyl Alcohol (PVA) as the surfactant. NLCs dispersion was characterized by particle size analysis, zeta potential, scanning electron microscopy (SEM), differential scanning calorimetry, and an in vitro release study. Results: Optimized NLCs loaded with TA were exhibited spherical shape with particle size 286.1 nm, polydispersity index 0.317, zeta potential-21.9 mV and entrapment efficiency 86.19% respectively. The result of differential scanning calorimetry (DSC) showed that drug was dispersed in NLCs in a crystalline state. In vitro release studies revealed that drug release of optimized batch was 8.34 % and 88.84% at 1h and 8h respectively. The release kinetics of the optimized NLCs best fitted the peppas-korsmeyer model. Furthermore, morphological investigations by SEM showed that optimized batch exhibit a spherical shape and a smooth surface. Conclusion: Thus, the results indicated that successfully prepared TA-loaded NLCs and could potentially be exploited as a carrier with improved drug loading capacity and sustained drug release. The present results demonstrated that these systems could be a promising platform for inflammatory diseases, in particular for psoriasis topical therapy.
ABSTRACT
Objective: The study aims at preparing the didodecyldimethylammonium bromide (DMAB)-modified PLGA nanoparticles (NPs) loading tetrandrine (Tet) (DMAB-Tet-PLGA-NPs) and investigating the preparation process, physicochemical characterization, in vitro cytotoxicity, and particle cellular uptake. Methods: DMAB-Tet-PLGA-NPs were prepared by the emulsion solvent diffusion method and the preparation process was optimized with the uniform design experiment. The drug loading, entrapment efficiency (EE), and in vitro drug release were studied to evaluate the drug-loading property. The in vitro cytotoxicity against human lung cancer cell A549 was measured by the standard MTT assay. The particles cellular uptake in A549 was evaluated by qualitative and quantitative methods. Results: DMAB-Tet-PLGA-NPs in the mean size of (205.40±2.66) nm with spherical shape and showed positive surface charge. Drug loading and EE were (2.130±0.035)% and (50.780±3.253)%, respectively. DMAB-Tet-PLGA-NPs could retard drug release in pH 7.4 release media and the cumulative release was up to 64.56% over 48 h. And DMAB-Tet-PLGA-NPs showed the significant dose-and time-dependent cytotoxicity of Tet in vitro and well cellular uptake by A549. Conclusion: DMAB-Tet-PLGA-NPs shows the good EE, uniform particle size, and could retard drug release in vitro. And DMAB-Tet-PLGA-NPs shows the significant cytotoxicity in vitro and well cellular uptake by A549.
ABSTRACT
Objective: To prepare tripterygium glycosides-loaded nanoparticles modified by 50% N-acetylated low molecular weight chitosan (LMWC-TG-NPs) and to investigate their in vitro release behavior. Methods: The LMWC-TG-NPs were prepared by modified self-emulsifying solvent diffusion method; The formulation of TG-NPs was optimized by orthogonal design and the modified condition of LMWC was determined based on the single factor analysis. The in vitro drug release of LMWC-TG-NPs was characterized with PBS (pH 7.4) containing 20% ethanol. Results: The optimized formulation of TG-NPs was as follows: Poloxamer 188 (1.0%), PLA (80 mg), organic phase (12 mL), and acetone-ethanol (2:3) were used to prepare TG-NPs suspension. The LMWC-TG-NPs were prepared by incubating TG-NPs suspension with 10% LMWC solution at the ratio of 1:1. The shape of the prepared LMWC-TG-NPs was spherical. The mean particle size, polydispersity index, entrapment efficiency, and drug loading were (207.6 ± 3.4) nm, 0.078 ± 0.009, (61.83 ± 2.43)%, and (10.70 ± 0.37)% (n=3), respectively. The in vitro release characteristics of LMWC-TG-NPs conform to Higuchi equation in PBS buffer composed of 20% ethanol at pH 7.4. Conclusion: The prepared LMWC-TG-NPs show a sustained-release characteristics with well-distributed particle size as well as high entrapment efficiency and drug loading, which could lay the foundation for the research on kidney targeting and toxicity.
ABSTRACT
OBJECTIVE: To prepare sustained-release microcapsules of metoprolol succinate(MS) and to investigate the influencing factors. METHODS: The sustained-release microcapsules of metoprolol succinate were prepared with ethyl cellulose(EC) in one step by the emulsion-solvent diffusion method. Uniform design was used to optimize the formulation and preparation technique. Its release behavior in vitro was studied. RESULTS: All microcapsules prepared under the optimum condition were spherical and smooth with the mean particle size in the range of 80-90 μm. The entrapment efficiency was 83.16% and drug release from the MS microcapsules during 18 h reached 96.1% in vitro. CONCLUSION: The microcapsules have good morphological characteristics, high entrapment efficiency and sustained-release effect in vitro.