FORMULATION, DEVELOPMENT AND CHARACTERISATION OF NIMODIPINE LOADED SOLID LIPID NANOPARTICLES

Objective: The aim of the present study is to develop solid lipid nanoparticles (SLNs) of Nimodipine using hot homogenization followed by ultrasonication technique and to improve the dissolution characteristics of the drug. Methods: The Nimodipine-loaded SLN was prepared using palmitic acid and stearic acid as a lipid matrix and Tween-80 as an emulsifier by a hot homogenization and ultra-sonication method. The physicochemical characteristics of SLN were investigated for entrapment efficiency, zeta potential, in vitro drug release, particle size analysis, Fourier transform infrared studies, scanning electron microscopy, and stability studies. Results: The mean particle size, PDI, Zeta potential and entrapment efficiency of optimized Nimodipine SLN formulation of stearic acid was found to be 119.54 nm, 0.165,-17.60mV, 85% and for palmitic acid was found to be 132.54 nm, 0.155,-17.0mV, 81% respectively. In vitro drug release studies indicated that after an initial burst release, SLN could provide prolonged release of Nimodipine. The selected SLNs have shown good stability for a period of 180 d. Conclusion: SLN formulations showed the best results in EE as well as in vitro drug release and therefore, these results indicate that SLN might be a promising delivery system to enhance the release of Nimodipine

DEVELOPMENT OF FAST-DISSOLVING TABLETS OF AMLODIPINE BESYLATE BY SOLID DISPERSION TECHNOLOGY USING POLOXAMER 407 AND POLOXAMER 188

Objective: Amlodipine besylate is a calcium channel blocker used in the treatment of hypertension which is practically insoluble in water. The present study aims to design oral fast-release tablets of amlodipine besylate and to optimize the dissolution of the drug by altering the carrier concentration.Materials and Methods: Poloxamer 407 (P407) and poloxamer 188 (P188) were selected as carriers for the preparation of solid dispersion (SD) by the solvent evaporation method with different drug-polymer ratios. The prepared SDs were evaluated for the physical state, drug:carrier interactions by X-ray diffraction (XRD), infrared spectroscopy, differential scanning calorimetry, and scanning electron microscopy.Results: From the dissolution studies, it is confirmed that all SDs showed increased dissolution rate when compared to pure amlodipine besylate. Among the two polymers used, P407 was found to be better than P188 in enhancing dissolution efficiency. The tablets were prepared using SD of amlodipine besylate containing P407 as a carrier. The results showed that P407 SD-based tablets gave a significantly higher release of amlodipine besylate when compared with control tablets. The infrared spectral studies showed that there was no significant interaction between amlodipine besylate and its formulation with different polymers used in the preparation of SDs. XRD studies revealed that the degree of crystallinity of amlodipine besylate reduced when the concentration of carriers increased, which reveals that the drug is in amorphous nature.Conclusion: The combination of SD technology and using superdisintegrants in the formulation is a promising approach for preparing efficient, fast-dissolving tablet of poorly water-soluble drugs, viz., amlodipine besylate

ARTIFICIAL NEURAL NETWORKS: FUNCTIONINGANDAPPLICATIONS IN PHARMACEUTICAL INDUSTRY

Artificial Neural Network (ANN) technology is a group of computer designed algorithms for simulating neurological processing to process information and produce outcomes like the thinking process of humans in learning, decision making and solving problems. The uniqueness of ANN is its ability to deliver desirable results even with the help of incomplete or historical data results without a need for structured experimental design by modeling and pattern recognition. It imbibes data through repetition with suitable learning models, similarly to humans, without actual programming. It leverages its ability by processing elements connected with the user given inputs which transfers as a function and provides as output. Moreover, the present output by ANN is a combinational effect of data collected from previous inputs and the current responsiveness of the system. Technically, ANN is associated with highly monitored network along with a back propagation learning standard. Due to its exceptional predictability, the current uses of ANN can be applied to many more disciplines in the area of science which requires multivariate data analysis. In the pharmaceutical process, this flexible tool is used to simulate various non-linear relationships. It also finds its application in the enhancement of pre-formulation parameters for predicting physicochemical properties of drug substances. It also finds its applications in pharmaceutical research, medicinal chemistry, QSAR study, pharmaceutical instrumental engineering. Its multi-objective concurrent optimization is adopted in the drug discovery process, protein structure, rational data analysis also

THERMOSENSITIVE HYDROGELS–A POTENTIAL CARRIER FOR THE DELIVERY OF DRUGS AND MACROMOLECULES

In this review, the authors have discussed scientific advances in thermosensitive hydrogels over the past two decades. The ability of the thermo-sensitive hydrogel to undergo rapid changes with response to temperature makes it an attractive candidate for many biomedical applications such as targeted drug delivery, wound healing, soft contact lenses, sensors, tissue regeneration, gene, and protein delivery. This review aims to deliver a brief overview of gelation properties, merits, and demerits of various natural and synthetic thermo-sensitive polymers that have significant clinical relevance. The report emphasizes the importance of injectable thermosensitive hydrogels, as it can offer improved solubility of hydrophobic drugs and site-specificity, extended-release of drugs and macromolecules, improved safety, and local administration of drugs. The authors has also provided a commentary on the delivery of drugs or macromolecules from thermo-sensitive hydrogels through various approaches. This review highlights the current status of research in thermo-sensitive hydrogels and emphasizes the importance of developing nontoxic thermo-sensitive hydrogels, dual responsive, and multi-responsive hydrogel systems

TRANSDERMAL DELIVERY OF CALCIUM CHANNEL BLOCKER: DEVELOPMENT AND CHARACTERIZATION

  Objective: Felodipine, a BCS class II calcium channel blocker, is used in the management of hypertension and angina pectoris. Due to the poor solubility and low bioavailability of the drug, there is a necessity to design an alternative route to achieve a constant plasma concentration of felodipine for its maximum therapeutic utility and can be achieved by transdermal route.Methods: In this study, matrix type transdermal patches were prepared using different combinations of hydrophilic polymer, namely, polyvinylpyrrolidone (PVP) and hydrophobic polymer, namely, ethyl cellulose (EC) by solvent evaporation technique and were subjected for characterization.Results: The Fourier transform infrared studies confirmed the compatibility between drug and polymers. Hydrophilic nature of the polymers greatly influenced physical characteristics and dissolution rate. Equal percentage of PVP and EC yielded patches with good folding endurance. The concentration of plasticizer present in the patches gave them desired folding endurance, and it increased with the presence of hydrophilic polymer. The formulation with highest PVP concentration, F3, exhibited a maximum drug release of 96.23% for 24 hrs. While the formulation with highest EC concentration, F5, exhibited only 74.45% drug release for 24 hrs.Conclusion: From the data, formulation F2 (PVP/EC, 2:1) can be concluded as best formulation due to its desired physical characteristics, good initial drug release, sustained release behavior, and good in vitro permeation. This formulation can be further studied in a clinical scenario

RECENT UPDATE ON ORAL FILMS: A BENCH TO MARKET POTENTIAL

Oral films are gaining a lot of attention as a substitute approach to the conventional dosage form. Over the past few years, many of the pharmaceutical scientists throughout the world are focusing their research on oral films, trying to see the sights of oral films as a novel drug delivery system. The oral films are convenient to swallow for geriatric and pediatric patients, are self-administrable, used for systemic and local action and rapid release of a drug, which makes it an excellent system of drug delivery. This review article mainly discusses the manufacturing aspects of films and their characterization, applications and the constraints in the development of oral films along with highlights of market potential

SCREENING AND OPTIMIZATION OF VALACYCLOVIR NIOSOMES BY DESIGN OF EXPERIMENTS

Objective: The objective of the study was to perform a screening, optimization of valacyclovir niosomal formulation to achieve a sustained release of drug using the design of experiments by 32 full factorial design.Methods: Valacyclovir loaded niosomes were prepared using thin film hydration method by varying the ratio of Span 60 and Cholesterol. The prepared niosomes were evaluated for vesicle size, entrapment efficiency, cumulative drug release, fourier transformed infrared spectroscopy (FTIR), zeta potential and surface morphology by field emission scanning electron microscopy (FESEM).Results: The valacyclovir was successfully encapsulated and its entrapment efficiency ranged from 36.70 % to 50.62 %. The average vesicle size of the niosomes was found to be 431 to 623 nm. At 8th hour the drug release varied from 77.50% to 96.31 %. The optimized niosomes were multilamellar with a surface charge potential of about-43.2 mV. The studies revealed that the interaction of cholesterol and surfactant had a substantial effect on vesicle size, entrapment efficiency and drug release from the niosomes. The release kinetics of the optimized niosomes followed zero order kinetics with fickian diffusion controlled mechanism. The stability studies were performed for the optimized formulation and found that the formulation is stable at 4°C ± 2°C.Conclusion: Model equations were developed for the responses. No significant difference was observed between the predicted and observed value, showing that the developed model is reliable

Evaluation of soluble ST2 as a novel cardiovascular biomarker in patients with acute myocardial infarction

Background: Soluble ST-2 has considerable prognostic value and is used as an aid for risk stratification in identifying patients who are at high risk of cardiovascular disease. The main objective of the study was to analyze the level of soluble ST-2 biomarker in patients with acute myocardial infarction and chronic stable angina patients and secondly to evaluate the cardiovascular outcomes after 30 days.Methods: A total of 71 patients were enrolled into the study, patients were divided into two groups of which 50 patients were in test group (AMI patients) and the remaining 21 patients were in the control group (chronic stable angina). Then, 5ml of blood was collected from the patients and plasma soluble ST-2 was estimated from the sample using ELISA technique. Patients were then followed up to 30 days to ascertain the development of major adverse cardiovascular outcomes.Results: The median concentration of soluble ST-2 in test group was found to be 213.46pg/ml and in control group was found to be 124.53 pg/ml. Soluble ST-2 correlated significantly with left ventricular ejection fraction (LVEF) between the two groups (P value=0.01). Measurement of soluble ST-2 early after MI assists in the prediction of adverse cardiovascular events. In this study, soluble ST-2 was found to be higher in patients with acute myocardial infarction and also in patients with poor ejection fraction.Conclusions: Soluble ST-2 is a novel cardiovascular biomarker that is elevated in patients with acute myocardial infarction

Developing the solid lipid nanoparticles of Losartan using the stearic acid and glyceryl monostearate as the carrier matrices

This research work deals with the design and development of the solid lipid nanoparticles of Losartan to improve solubility of poorly soluble drug. Losartan solid lipid nanoparticles are formed using hot homogenization technique followed by ultrasonication technique. Experiment trend is predicted using the standard calibration curve. The parameters studied are the percent drug release, entrapment efficiency, particle size of SLN and the in-vitro drug release of prepared SLN. The results obtained in this research work clearly indicated that the developed solid lipid nanoparticle delivery system for the highly lipophilic drug, Losartan using stearic acid, glyceryl monostearate as carrier matrices can be used effectively for hypertension