A Short Review on Application of Liquisolid Technology

In this paper we have surveyed about formulation and evaluation of Liquisolid formulations and its work in antidiabetics . Mostly poorly water soluble drugs are in research category despite of less dissolution rate and poor bioavailability. Solubility is a vital parameter to develop new formulation as industries faced serious issue regarding the poor aqueous solubility of the drugs. Various methods for solubility enhancement include modifications of the drug, involvement of co-solvents, complexation, salt formation, size reduction. A propitious technique to solve major challenges like solubility, dissolution rate and their bioavailability. This technique can be defined as the conversion of poorly soluble liquid medications into non-adherent, dry, compressible and free flowing powder mixtures with help of excipients. Many anti-diabetic drugs are belonging to BCS Class-II facing challenges like solubility and bioavailability.

Solubility Study of Acetylsalicylic Acid in Ethanol + Water Mixtures: Measurement, Mathematical Modeling, and Stability Discussion

Solubility determination of poorly water-soluble drugs is pivotal for formulation scientists when they want to develop a liquid formulation. Performing such a test with different ratios of cosolvents with water is time-consuming and costly. The scarcity of solubility data for poorly water-soluble drugs increases the importance of developing correlation and prediction equations for these mixtures. Therefore, the aim of the current research is to determine the solubility of acetylsalicylic acid in binary mixtures of ethanol+water at 25 and 37°C. Acetylsalicylic acid is non-stable in aqueous solutions and readily hydrolyze to salicylic acid. So, the solubility of acetylsalicylic acid is measured in ethanolic mixtures by HPLC to follow the concentration of produced salicylic acid as well. Moreover, the solubility of acetylsalicylic acid is modeled using different cosolvency equations. The measured solubility data were also predicted using PC-SAFT EOS model. DSC results ruled out any changes in the polymorphic form of acetylsalicylic acid after the solubility test, whereas XRPD results showed some changes in crystallinity of the precipitated acetylsalicylic acid after the solubility test. Fitting the solubility data to the different cosolvency models showed that the mean relative deviation percentage for the Jouyban-Acree model was less than 10.0% showing that this equation is able to obtain accurate solubility data for acetylsalicylic acid in mixtures of ethanol and water. Also, the predicted data with an average mean relative deviation percentage (MRD%) of less than 29.65% show the capability of the PC-SAFT model for predicting solubility data. A brief comparison of the solubilities of structurally related solutes to acetylsalicylic acid was also provided.

Pathfinder Nanosponges for Drug Targeting by Factorial Design: A Glance Review

For a long time, drug delivery systems (DDS) have been targeted to get expected results. With nanotechnology-based DDS, a wide assortment of flawless challenges can be tackled at present. Known as a nanosponge, a nanosponge is a modern division of material consisting of tiny particles that transmit only a few nanometers. The nano-formulations are highly effective for the delivery of low-solubility drugs. Many drugs with narrow therapeutic windows can benefit from improving water solubility. It has even been claimed they can be utilized to target and control delivery. In addition, huge amounts of money have been spent on developing new formulations of the DDS in recent times. Learn how nanosponges are prepared, its advantages, and its disadvantages. Resources were consulted to comprehend recent enhancements and patents in the domain. The ideal DDS has been developed by combining many different formulations; nano sponges are one of them. Analysts have examined them and found that they produce positive results and can improve the stability of poorly water-soluble drugs. The drug will be released at the precise target site when it reaches the body and sticks to the surface of the target site. As medication maximum action declines, it is more difficult to formulate impotent drugs. Considering this, nanosponges are organized and examined to determine whether they are problematic. Nanosponges in drug delivery can be characterized by their characteristics, preparation, factors, and applications. The article was written based on research articles about nanosponges. Data on nanosponges drug delivery systems from the past decade was collected using a factorial design. Study authors report that factor design plays an imperative role in optimizing drug dosage forms. Researchers will save time by reviewing the literature on nanosponges via factorial designs instead of searching for it.

Review on Polymer Based Nanoparticles for Increase the Bioavalibilty of Poorly Water Soluble Drug

In this review study about the polymeric nanoparticles and how polymer based nanoparticles increase bioavailability of less water soluble drugs. Polymeric nanoparticles have a matrix of biodegradable and biocompatible polymers of synthetic and natural origin. Polymer based nanoparticles are very useful for increase the solubility of the poor water-soluble drugs by decrease the particles size. Polymeric nanoparticles are very useful for targeting the drug to the specific site. Polymeric nanoparticles are also used to maintain and control the release of the drug. In present review study on the type of polymer used for the preparation of the polymer based nanoparticles. The choice of method depends on a number of factors, such as, particles size, area of application and characterization of polymeric nanoparticles.

Formulation, Development and Characterization of Floating Microspheres of Selected Calcium Channel Blocker

The main aim of the present investigation is to study of formulation, development and characterization of floating mcrospheres of verapamil hydrochloride. Floating microspheres with a central hollow cavity were prepared by using a modified Quasi-emulsion diffusion technique. Weighed quantities of verapamil hydrochloride, ethyl cellulose, polyethylene oxide and hydroxy propylmethyl cellulose (HPMC K15M) were dissolved in a mixture of ethanol and dichloromethane (1:1 solvent ratio) at room temperature in a magnetic stirrer at 50 rpm for 50 min. The samples were assayed for drug content using UV spectrophotometer at 228 nm after suitable dilution. No interference was found due to the other components of floating microspheres at 228 nm. The yield was determined by weighing the microspheres and then the percentage yield was calculated with respect to the weight of the input materials, i.e., weight of verapamil and polymers used. The polymers like ethyl cellulose, eudragit L 100, polyethylene oxide and HPMC were selected for hollow microspheres preparation. These formulations contained ethyl cellulose (2%) and Polyethylene oxide (1%), HPMC K15M (1%) & eudragit L100 (1%) respectively. The encapsulation efficiency ranged between 53 ± 2.2 to 89 ± 1.9%, and was observed that the encapsulation efficiency increased with increasing amount of polymers in the hollow microspheres. The sphericity factors for all formulations were in the range of 1.01 ± 0.2 to 1.29 ± 0.6 and the sphericity values of best formulations F3, F7 and F9 were 1.05±0.2, 1.07 ± 0.1 and 1.16 ± 0.1 respectively. Quassi emulsion method used for preparation of hollow microspheres was suitable for poor water soluble drugs, because the drug was soluble in the internal organic phase.

Eco-friendly and Economical Spectrophotometric Estimation of the Low Water-Soluble Drug (Norfloxacin) Applying the Concept of Mixed Hydrotropy

Objectives The main aim of the research was to analyze an economical and eco-friendly approach to improve the solubility of norfloxacin. The current analysis was to utilize the hydrotropic solutions to extract the drugs from their dosage forms, avoiding the use of costlier and harmful organic solvents. Materials and Methods In this study, an ultraviolet–visible spectrophotometer (model 1800, Shimadzu Corporation) was used to analyze the norfloxacin drug. The mixed hydrotropy approach was used to determine the solubility of norfloxacin. In this work, a blend solution (20% of urea + 20% of sodium benzoate) was used as a hydrotropic solubilizing agent. Results The solubility of norfloxacin drug in water was very low at ∼0.88 mg/mL and the solubility of norfloxacin drug in the blend solution was 11 mg/mL. From 98.96 (tablet II) to 99.35 (tablet I), the percent estimation value was achieved. This value was nearly 100, so the proposed method was correct. Standard deviation (0.2540–0.4156), percentage coefficient of variation (0.2566–0.4183), and the value of standard error (0.1481–0.2415) are also very low; hence, we can say that the proposed method is accurate. Conclusion To avoid the use of organic solvents, the mixed hydrotropy concept can be used for spectrophotometric estimation of low water-soluble drugs from bulk drug samples. It provides an economical and environmentally friendly mechanism.

Berberine-Loaded Biomimetic Nanoparticles Attenuate Inflammation of Experimental Allergic Asthma via Enhancing IL-12 Expression

Asthma is one of the most common chronic pulmonary disorders, affecting more than 330 million people worldwide. Unfortunately, there are still no specific treatments for asthma so far. Therefore, it is very important to develop effective therapeutics and medicines to deal with this intractable disease. Berberine (Ber) has fabulous anti-inflammatory and antibacterial effects, while its low water solubility and bioavailability greatly limit its curative efficiency. To improve the nasal mucosa absorption of poorly water-soluble drugs, such as Ber, we developed a platelet membrane- (PM-) coated nanoparticle (NP) system (PM@Ber-NPs) for targeted delivery of berberine to the inflammatory lungs. In vivo, PM@Ber-NPs exhibited enhanced targeting retention in the inflammatory lungs compared with free Ber. In a mouse model of house dust mite- (HDM-) induced asthma, PM@Ber-NPs markedly inhibited lung inflammation, as evident by reduced inflammatory cells and inflammatory cytokines in the lung compared with free Ber. Collectively, our study demonstrated the inhibitory actions of nasally delivered nanomedicines on HDM-induced asthma, primarily through regulating Th1/Th2 balance by enhancing IL-12 expression which could potentially reduce lung inflammation and allergic asthma.

Liquisolid Compacts Technique of Poor Water Soluble Drugs: An Overview

Liquisolid technique is new and promising method that can use to enhance the dissolution rate of poorly water soluble drugs. Liquisolid compact technique is based upon the dissolving the drug in a suitable non-volatile solvent by using carrier and coating material for the conversion of acceptable flowing and compressible powders. By applying the mathematical models the carrier and coating materials optimized. In this case the drug is almost solubilised in the solvent or molecularly dispersed state which contributes the enhanced drug dissolution.

Effect of Surfactants and Polymers on the Dissolution Behavior of Supersaturable Tecovirimat-4-Hydroxybenzoic Acid Cocrystals

(1) Background: Pharmaceutical cocrystals have attracted remarkable interest and have been successfully used to enhance the absorption of poorly water-soluble drugs. However, supersaturable cocrystals are sometimes thermodynamically unstable, and the solubility advantages present a risk of precipitation because of the solution-mediated phase transformation (SMPT). Additives such as surfactants and polymers could sustain the supersaturation state successfully, but the effect needs insightful understanding. The aim of the present study was to investigate the roles of surfactants and polymers in the dissolution-supersaturation-precipitation (DSP) behavior of cocrystals. (2) Methods: Five surfactants (SDS, Poloxamer 188, Poloxamer 407, Cremophor RH 40, polysorbate 80) and five polymers (PVP K30, PVPVA 64, HPC, HPMC E5, CMC-Na) were selected as additives. Tecovirimat-4-hydroxybenzoic (TEC-HBA) cocrystals were chosen as a model cocrystal. The TEC-HBA cocrystals were first designed and verified by PXRD, DSC, SEM, and FTIR. The effects of surfactants and polymers on the solubility and dissolution of TEC-HBA cocrystals under sink and nonsink conditions were then investigated. (3) Results: Both the surfactants and polymers showed significant dissolution enhancement effects, and most of the polymers were more effective than the surfactants, according to the longer Tmax and higher Cmax. These results demonstrate that the dissolution behavior of cocrystals might be achieved by the maintained supersaturation effect of the additives. Interestingly, we found a linear relationship between the solubility and Cmax of the dissolution curve for surfactants, while no similar phenomena were found in solutions with polymer. (4) Conclusions: The present study provides a basis for additive selection and a framework for understanding the behavior of supersaturable cocrystals in solution.