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1.
Curr Drug Deliv ; 7(1): 44-50, 2010 Jan.
Article in English | MEDLINE | ID: mdl-20044909

ABSTRACT

Repaglinide solid lipid nanoparticles (RG-SLN) were fabricated using stearic acid as lipid. Pluronic F68 (PLF68) and soya lecithin were used as a stabilizer. SLNs were prepared by modified solvent injection and ultrasonication methods. SLNs prepared with modified solvent injection method have larger particle size (360+/-2.5nm) than prepared with ultrasonication method (281+/-5.3nm). The zeta potential of the prepared formulations by these two methods varied from - 23.10 +/-1.23 to -26.01 +/-0.89 mV. The maximum entrapment efficiency (62.14 +/-1.29%) was obtained in modified solvent injection method. The total drug content was nearly same (98%) in both the methods. In vitro release studies were performed in phosphate buffer (pH 6.8) with 0.5% sodium lauryl sulphate (SLS) using dialysis bag diffusion technique. The cumulative drug release was 30% and 50% within 2 hrs in modified solvent injection and ultrasonication method, respectively. This indicates that RG-SLN prepared from modified injection method released the drug more slowly than SLNs prepared with ultrasonication method. Differential scanning calorimetry indicates that repaglinide (RG) entrapped in the solid lipid nanoparticles (SLN) exist in an amorphous or molecular state. Repaglinide loaded solid lipid nanoparticles prepared with both methods were of spherical shape as observed by transmission electron microscopy (TEM). These results suggest that modified solvent injection method is more suitable for preparation of repaglinide SLNs using stearic acid.


Subject(s)
Carbamates/chemistry , Drug Carriers , Hypoglycemic Agents/chemistry , Lipids/chemistry , Nanostructures , Piperidines/chemistry , Biological Availability , Calorimetry, Differential Scanning , Carbamates/pharmacokinetics , Hypoglycemic Agents/pharmacokinetics , Microscopy, Electron, Transmission , Particle Size , Piperidines/pharmacokinetics
2.
AAPS PharmSciTech ; 10(3): 716-23, 2009.
Article in English | MEDLINE | ID: mdl-19479385

ABSTRACT

The aim of the paper was to develop satranidazole-containing mucoadhesive gel for the treatment of periodontitis. Different mucoadhesive gels were prepared, using various gelling agents like sodium carboxymethylcellulose (SCMC), poloxamer 407, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, and the mucoadhesive polymer carbopol 934P. The selected formulations (based on the mucoadhesive force) were studied for different mechanical properties, such as mucoadhesive strength, hardness, compressibility, adhesiveness, and cohesiveness through Texture Profile Analyzer. In vitro satranidazole release from the prepared formulations was also determined and compared with marketed preparation of metronidazole (Metrogyl gel). The formulation SC30 (containing SCMC 3% w/v) showed maximum mucoadhesive strength (167.72 +/- 3.76 g) and adhesiveness (-46.23 +/- 0.34 N mm), with low hardness (9.81 +/- 0.04 N) and compressibility (40.05 +/- 0.48 N mm) and moderate cohesiveness (0.87 +/- 0.01). SC30 formulation exhibited long-term release. Thus, SC30 gel was evaluated for its clinical effectiveness along with marketed metronidazole gel. At the end of the study (42 days of clinical studies), both formulations were found to significantly reduce the probing depth, plaque index, gingival index, calculus criteria, and bleeding index. However, the SC30 gel was more effective in reducing the above parameters than marketed metronidazole gel. This study confirmed the acceptability and effectiveness of satranidazole gel for treatment of periodontitis.


Subject(s)
Anti-Bacterial Agents/administration & dosage , Anti-Bacterial Agents/therapeutic use , Nitroimidazoles/administration & dosage , Nitroimidazoles/therapeutic use , Periodontitis/drug therapy , Adhesiveness , Adhesives , Anti-Bacterial Agents/chemistry , Chemistry, Pharmaceutical , Delayed-Action Preparations , Excipients , Female , Gels , Gingiva/pathology , Gingivitis/pathology , Hardness , Humans , Kinetics , Male , Nitroimidazoles/chemistry , Periodontitis/pathology , Solubility , Young Adult
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