Formulation and Evaluation of Nanosuspension as an Alternative Approach for Solubility Enhancement of Simvastatin

Solubility is an essential factor for drug effectiveness. Simvastatin is poorly water-soluble drug and its bioavailability is very low. Nanosuspension is one of those approach which can tremendously enhance the effective surface area of drug particles by reducing the particle size and there by increases the rate of dissolution and hence improve bioavailability. The main purpose of the present investigation was to increase the saturation solubility of simvastatin by preparation of nanosuspension. Nanosuspension of simvastatin were prepared by nanoprecipitation method using hydroxypropyl cellulose as stabilizer and sodium lauryl sulphate as surfactant. Prepared nanosuspension was evaluated for its particle size, total drug content, entrapment efficiency and saturation solubility study. On the basis of the evaluation, the best batch F8 formulation demonstrated highest drug content and entrapment efficiency with average particle size of 0.004µm. The saturation solubility studies show the solubility of the prepared nanosuspension has increased as compared to the pure drug due to the particle size reduction. The nanosuspension of simvastatin could be successfully prepared and can be concluded that the nanosuspension formulation is a promising approach to enhance the solubility. The nanoprecipitation is a simple and effective method to produce nano sized particles of poorly water-soluble drugs with enhance solubility.

Enhancement of Solubility Ibuprofen by Solid Dispersion Technique on Natural Mucilage

In this study generally solid dispersions (SDs) of ibuprofen were prepared by for all intents and purposes melt dispersion technique using natural mucilage of Lemon seed as carrier, which really is quite significant. Physical mixtures (PMs) of ibuprofen literally were also prepared with the same carrier and in the same drug-carrier ratio (1:0.5, 1:1 and 1:1.5) to compare the dissolution profile, which generally is fairly significant. The solid dispersions and kind of physical mixtures for all intents and purposes were investigated for drug loading, saturation solubility and dissolution behavior in a subtle way. Saturation solubility study really actually was basically carried out in phosphate buffer (pH 7.4), 0.1 N HCL solution and distilled water, which kind of literally is quite significant. Solid dispersions for all intents and purposes particularly were mostly really found definitely fairly effective to literally kind of enhance the solubility of ibuprofen significantly in all the media, which actually is quite significant. Dissolution test specifically was mostly carried out in two different media, phosphate buffer (pH 7.4) and 0.1 N HCL. Solid dispersion containing Lemon seed mucilage at the ratio of 1:1.5 (drug: carrier) basically showed faster and sort of definitely higher drug release and basically was specifically really found to for the most part actually be most sort of effective among all the very actually solid dispersions in a generally big way, which kind of is fairly significant. Drug carrier interactions specifically specifically were studied by comparing Fourier definitely mostly Transform generally Infrared Spectroscopy (FT-IR) of particularly solid dispersions with pure drug which essentially revealed that the SDs specifically were kind of really stable in a pretty big way, which is fairly significant. So, fairly very solid dispersion may particularly be an definitely really effective technique to specifically enhance dissolution rate of ibuprofen, which kind of literally is fairly significant in a fairly big way.

Formulation and Evaluation of Lamivudine Nanosuspension

The present research aimed to develop & Evaluation of Lamivudine Nanosuspension. Lamivudine is a potent in vitro inhibitor of human immune deficiency virus belongs to the category of anti-retroviral drugs. The formulated Nanosuspension was subjected to various evaluation parameters like particle size, polydispersity index, zeta potential, drug content, viscosity, saturation solubility studies, In vitro release, treatment of kinetic data, and stability studies. The polydispersity ranged from 0.218 PDI to 0.331 PDI and zeta potential ranged from -1.60 mV to -4.79 mV are the important evaluation parameters are responsible for the stability of nanosuspensions. The Polydispersity index presents the quantity of particle size distribution ranges from 452.4 nm to 532.2 nm. In this result, LNSF4 shows spectacular drug content range of 86±1.8% to 97±2.5% it is the maximum drug content. The Brook field viscometer to determine the viscosity of Lamivudine Nano suspension of different formulations was found to be 44.4±2.1 cps to 87.7±1.4 cps. The general Nanosuspension formulations LNSF4 shows 98.64 % better controlled released in comparison with abundant formulation. In all the cases the best-fit model encounter uoto be peppas with ‘n’ value between 0.768 to 0.917. The ‘n’ value of formulation LNSF4 was 0.876 and suggesting so the drug was released by Zero-order kinetics. Acceleration stability studies intermediate storage condition has been changed from 30°C ± 2°C and 60% RH ± 5% Relative Humidity. After a 90 days study it revolves that there’s no change in Drug content, In vitro drug release, and particle size. Keywords: Lamivudine, Nanosuspension, Saturation solubility, Scanning Electron Microscopy, Stability study.

Development of Oral Chewable Tablets Containing Montelukast Nanoparticles for the Treatment of Childhood Asthma: Preclinical Study in Animal Model

The aim of the present study was to formulate oral chewable tablets of Montelukast (MTL) in the form of nanoparticles (NP’s). The MTL loaded NP’s were formulated by ionotropic external gelation method using tripolyphosphate (TPP) as crosslinking agent and Tween 60 as surfactant. NP’s were characterized for drug loading, encapsulation efficiency, surface morphology, saturation solubility, particle size, zeta potential and polydispersity index. The optimized NP formulation was used for development of chewable tablets using direct compression method. The prepared tablets were characterized for disintegration test, dissolution, thickness, hardness, friability and assay. The optimized formulation was evaluated in asthamatic animals to demonstrate the efficiency in asthama. The encapsulation efficiency of NP’s was found between 91.24 to 98.21% while drug loading was in the range of 10.09–14.25%. All formulations were found of nanosized in nature (110 to 200 nm) with excellent zeta potential (20.12 to 22.27 mV). PDI of all NP formulations were found within acceptable limit (less than 0.3). The nanoparticles were found spherical in shape with smooth surface. The saturation solubility of MTL was enhanced nearly 10 times (92 mg/ml) as compared to pure MTL saturation solubility. All physical parameters of the tablets were found within range. The optimized tablets showed disintegration time of 20 sec while other formulations showed DT in the rage of 35–57 sec. Tab1 (Optimized formulation) showed almost 100% MTL release from chewable tablets within the period of 30 min. Reduction in lung resistance (RI) was found in animals treated with Tab1. This reduction in RI was found nearly two fold and three fold as compare to MTL treated and control group animals. These observations clearly support the efficacy of chewable tablets containing nanoparticulate MTL in asthmatic animals.

Study Evaluation Maternity Nutrition and Pregnancy In Vitro and In Vivo—Progesterone Nanocrystal Injection

In this study, the insoluble drug, progesterone, was formulated into a progesterone nanocrystal injection to improve the saturation solubility, release rate, and efficacy of progesterone, as well as to increase the relative bioavailability of progesterone, reduce the subsequent irritation, and minimize the toxicity; the advantages and feasibility of the progesterone nanocrystalline injection in the prevention of premature delivery and protection against pregnancy-associated risks in pregnant females was evaluated. The wet grinding method was used to prepare the progesterone nanocrystalline injection; its morphology, particle size, and potential were characterized by transmission electron microscopy. Crystal structure was analyzed by X-ray powder diffraction; the solubility of the injection and the progesterone drug substance in water, and the In Vitro release of the drug were evaluated for its nanometer effect In Vitro. Rabbits were injected with the progesterone nanocrystal injection as well as commercially available progesterone injections for evaluation in vivo. The formulation process of a progesterone nanocrystal injection is feasible. The crystal form is stable and the particle size is uniform. Moreover, we found that it improves the release rate, saturation solubility, and bioavailability of progesterone, while reducing muscle irritation. The results have clinical research significance.

IMMEDIATE RELEASE SOLID DISPERSION TABLET OF AZILSARTAN: FORMULATION STRATEGY TO ENHANCE ORAL BIOAVAILABILITY

Objective: Objective of the present study was to develop an immediate release solid dispersion tablet to enhance oral bioavailability of Azilsartan. Methods: Solid dispersion of azilsartan was developed using Soluplus® as a novel solubility enhancer by the solvent evaporation technique. 32factorial design was used in a fully randomized order to study effect of amount of azilsartan and Soluplus on solubility (µg/ml) and % drug dissolved in 30 min. Prepared solid dispersion was evaluated for different micromeritic properties, saturation solubility, and wettability. Then solid dispersion of all the batches compressed into an immediate-release tablet using sodium starch glycolate as a super disintegrant. Developed tablet formulations were evaluated for various post-compression parameters and satisfactory formulation among these were further studied for Fourier-transform infrared spectroscopy (FTIR), Differential Scanning Colorimeter (DSC), X-Ray Diffraction (XRD), in vivo absorption and stability study. Results: Results of micromeritic properties of solid dispersion showed that good flowability, compressibility, wettability, and saturation solubility. Post compression parameters of immediate-release tablets were found to be in acceptable limits. Batch ASD2 containing 40 mg Diacerein and 80 mg of Soluplus showed maximum drug release i.e. 99.82 % within 30 min. Compatibility study using FTIR, DSC, and XRD showed that drug is compatible with Soluplus. In vivo absorption study showed that, 2.67 fold increase in Area Under Curve (AUC) as compared to plain Azilsartan. Relative bioavailability was found to be 267.11 %. Results of stability study indicate that developed formulations were stable at accelerated temperature and humidity conditions. Conclusion: Study concluded that solid dispersion using Soluplus as a solubility enhancer is a suitable formulation strategy to enhance solubility, dissolution, and bioavailability of poorly water-soluble drug-like Azilsartan.

Central composite designed solid dispersion for dissolution enhancement of fluvastatin sodium by kneading technique

Aim: This research is focused on enhancing aqueous solubility and dissolution of fluvastatin sodium (FSS) through solid dispersion (FSS-SD) production using polyethylene glycol 6000 and polyvinyl pyrollidone K-30 by kneading technique. Methodology & results: Central composite design explored the influence of polyethylene glycol 6000 and polyvinyl pyrollidone K-30 on T50% and Q90. The aqueous saturation solubility of FSS (8.7 ± 1.12 μg/ml) was amplified 20-fold in FSS-SD (179 ± 4.16 μg/ml). Cumulative drug release from FSS and optimized FSS-SD were 27.49 and 87.4% within 90 min, respectively. Conclusion: FSS-SD production using kneading technique offers great prospective in maximizing FSS's solubility and dissolution.

Symurban Nanocrystals for Advanced Anti-Pollution Skincare

Several of most common dermatoses worldwide, e.g., psoriasis and atopic dermatitis, are worsened in their clinical picture when the skin is regularly exposed to an increased air pollution level, e.g., particulate matter. This is explainable by the activation of the aryl hydrocarbon receptor (AhR) in the skin, which results in an increased release of proinflammatory cytokines and matrix metalloproteinases. Symurban is a competitive AhR antagonist and thus allows the effective protection of skin. In order to improve its dermal bioavailability as a poorly soluble active agent (0.25 µg/mL), nanocrystals were prepared and evaluated. Nanocrystals are pure active crystals reduced in particle size to the submicron range of 100 to 1000 nm. They feature the properties of nanocrystals, such as increased saturation solubility and dissolution velocity, without having to be declared as nanomaterial. Production methods and parameters were systematically investigated. Wet bead milling at 2000 rpm for 30 min yielded the best results. A z-average of 280 nm was achieved for a 10% Symurban suspension with a polydispersity index of 0.20, indicating a narrow size distribution. For the long-term stabilization of the nanocrystal suspension, the performance of 15 surfactants of different categories and HLB values were investigated and evaluated. It was found that non-ionic surfactants in general were better able to stabilize the system than anionic or amphoteric surfactants. Highest stability of over 12 months at 25 °C was achieved with 2% Plantacare 810 UP, an ECOCERT surfactant with high skin tolerance. The suspension was also chemically long-term stable with >97% of remaining Symurban over 12 months. The saturation solubility of Symurban as nanocrystals was significantly increased from 0.25 to 2.9 μg/mL, which corresponds to a factor of >11. In a case study of one male volunteer with healthy skin conditions, penetration profiles of Symurban nanocrystal hydrogel and commercial anti-pollution serum containing an identical amount of Symurban were determined and compared. After 20 min of exposure, the relative Symurban concentration in the deeper skin layers (tape 19-30) was more than two times higher for nanocrystal hydrogel (16%) than the commercial serum (7%). These results suggest that nanocrystals are a promising delivery system for the poorly soluble anti-pollution agent Symurban.