Rosuvastatin is a lipid lowering agent, which has low solubility and low bioavailability of 20% with oral administration. Therefore the present study was undertaken to improve solubility and bioavailability of Rosuvastatin by formulating it into Nano structured lipid carriers (NLCs) by using stearic acid and Compritol ATO 888 as solid-lipid, Oleic acid as liquid-lipid and Poloxamer 188 as a surfactant. Rosuvastatin loaded NLCs were prepared by high shear homogenisation followed by Ultra sonication technique. In this study two solid lipids (stearic acid and Compritol ATO 888) were compared with liquid lipid in different concentration in order to select suitable solid liquid lipid for Rosuvastatin to achieve particle size in nano range. The prepared NLCs were evaluated for particle size and size distribution, Poly dispersity index, drug content, entrapment efficiency, zeta potential, In-vitro drug release, In-vivo bioavailability study in rat. The drug content for the formulation F1 to F8 was found to be in the range of 83.18 to 96.59%. The formulation F3 was optimised based on the mean particle size, poly dispersity index, entrapment efficiency and zeta potential which showed 213.26 nm, 0.22, 89.1% and -50.6 respectively. Transmission electron microscopy (TEM) studies on formulation F3 revealed that all the particles were within the nano size range. Formulation F3 showed In-vitro drug release of 76.22% at the end of 12 hrs with a sustained release. HPLC method was developed for determination of Rosuvastatin calcium in rat plasma for bioavailability and pharmacokinetic evaluation. The relative bioavailability of NLC formulation F3 showed an enhanced bioavailability with two folds as compared to the marketed conventional tablet. The stability study was carried at 4ºC with 65% RH for 30 days showed no change in the particle size, entrapment efficiency and In-vitro drug release.
Introduction: Quinine Sulphate is an antimalarial agent usually indicated in the treatment of chloroquine resistant malaria. Objective: The objective of the present investigation was to prepare quinine sulphate loaded solid lipid nanoparticles by ultrasonic solvent emulsification technique using different surfactants (Tween 80, Poloxamer 407, Poloxamer 188) in order to mask the bitter taste, thereby improving patient compliance and to provide dose precision and a flexible system that allows dose adaptation according to the body weight. Method: Glyceryl monostearate was used as a lipid (drug to lipid ratio 1:3). The prepared solid lipid nanoparticles were characterized for various parameters like particle size and shape, zeta potential, entrapment efficiency, In vitro evaluation of taste masking efficiency, In vitro drug release, In vitro drug release kinetics. Results and discussion: The mean hydrodynamic diameter of the particle decreased whereas the entrapment efficiency increased with an increase in the surfactant concentration. Higher surfactant concentration showed faster In vitro release. The formulations showed negligible release at pH 6.8 and almost 100% release at pH 1.2, which is desirable so as to mask the taste by delaying the release during administration without hampering the drug release in stomach. Formulation F9 containing 2% w/v poloxamer 188 was selected as the optimized formulation as it showed high entrapment efficiency and negligible release in Simulated Salivary Fluid (SSF) pH 6.8 when compared to pure drug but showed almost 100% release at pH 1.2. Conclusion: It can be concluded that quinine sulphate was proven to be a suitable candidate for formulating solid lipid nanoparticles to achieve better patient compliance among pediatric and geriatric populations by masking the bitter taste and avoiding the difficulty in swallowing.
The objective of this research work was to develop a simple, rapid and reliable HPTLC method for standardization of anti-diabetic polyherbal formulation and to carry out validation of Trigonelline in formulation. Development of method was carried out by using Quercetin, Gallic Acid, Curcumin and Trigonelline as bioactive markers reported to have an anti-diabetic activity. Chromatographic analysis was performed using silica gel 60 F 254 TLC plate, CAMAG Linomat 5 applicator and solvent system consisting of Isopropyl Alcohol: Ammonia: Acetone in the ratio 1:1:1. Densitometry scanning was performed under reflectance absorbance mode at 254 nm and 366 nm to identify the spots. R f value of the marker compounds Quercetin, Gallic Acid, Curcumin and Trigonelline was found to be 0.66, 0.42, 0.81 and 0.34 respectively. Validation of Trigonelline was carried out in formulation as per ICH guidelines in terms of Linearity, Precision, Repeatability, Specificity, Robustness, LOD, LOQ and Accuracy. No analytical method has been reported so far associated with a polyherbal formulation containing Quercetin, Gallic acid, Curcumin and Trigonelline focusing on anti diabetic activity. Thus this method can be used for routine quality control of raw material as well as formulation containing Trigonelline as one of its component.
Aim: The objective of the present study was to develop and evaluate cefixime nanosuspension to enhance its oral bioavailability. Materials and Methods: The method used was solvent/ antisolvent method in which methanol and Millipore water was used as solvent and antisolvent respectively. The surfactants used for the preparation were PVP K30 and HPMC K100 which was found to be compatible in the formulation. Compatibility of the drug and drug with its excipients was found out by FTIR studies. Characterization of the optimized Cefixime Nanosuspension was carried out by particle size analysis, Differential Scanning Calorimetry, Zeta Potential, Drug content, in-vitro drug release studies, Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy(TEM). The antimicrobial activity of cefixime nanosuspension was done by Disk diffusion method against E. coli performed in nutrient agar with different concentrations of the formulation. The Minimum Inhibitory Concentration (MIC) was determined by calculating Zone of inhibition. A method was developed forcefixime nanosuspension and validated by High Performance Thin Layer Chromatography (HPTLC). Results: The optimizedcefixime nanosuspension was validated for Identification, Linearity, Specificity, Precision and Recovery. The Recovery of cefixime nanosuspension was found to be 95.57%.
In past decades poly lactic-co-glycolic acid (PLGA) has been one of the most attractive polymeric candidates used to fabricate devices for diagnostics and other applications of clinical and basic science research, including vaccine, cancer, cardiovascular disease, and tissue engineering. In addition, PLGA and its co-polymers are important in designing nanoparticles with desired characteristics such as biocompatibility, biodegradation, particle size, surface properties, drug release and target ability and exhibit a wide range of erosion times. PLGA has been approved by the US FDA for use in drug delivery. This article represents the more recent successes of applying PLGA-based nanotechnologies and tools in these medicine-related applications, and factors affecting their degradation and drug release. It focuses on the possible mechanisms, diagnosis and treatment effects of PLGA preparations and devices.
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