Novel Approaches to Enhance Oral Bioavailability of Poorly Soluble Drugs

Oral administration is considered as major, convenient route among all other routes of delivery, owing to several benefits. But, the poor solubility or enzymatic/metabolic activity are the major concerns in developing a successful formulation. About 40% of approved drugs which are in the current market and 90% of new drug molecules in the developmental pipeline are hydrophobic in nature. The challenge to formulate insoluble drugs has met with various approaches to overcome the problems related to solubility, application of nanotechnology is one amongst them. The present review deals with various nanocarriers and technologies that are proven to be effective in enhancing the bioavilability of poorly soluble drugs.

Utilization of Lipids, Polymers by Modern Techniques for Innovative Pharmaceutical Formulations and Medical Devices

With advancing science and technology, new futuristic technologies have been upcoming that are having a greater impact on the pharmaceutical and biomedical fields. Many lipids and polymer of natural and synthetic origin have spread horizons enabling to reach in fabricating delivery systems for unmet medical needs. In this modern biomedicine era, we must outline and scrutiny the roles of these biomaterials and the modern technologies that are shaping up the advancing medicines. The real challenges in modulating, fine-tuning the biomaterials for their bioactive properties are vital for assessing the in-vivo performance of the developed systems. Therefore, the present review discusses the detailed analysis of the current research reported in the technologies of utilizing the lipids, polymers, and their role in delivering the drugs, genes, and designing advanced implantable medical devices. The scrutiny also focuses on key optimization tools, analytical methods, formulation, and biomedical techniques helpful in developing the solutions that can be administered different routes in different therapeutic indications.

Formulation and in-vitro evaluation of ciprofloxacin HCL floating matrix tablets

Oral drug delivery is the most widely utilized route of administration among all the routes that have been explored for systemic delivery of drugs via pharmaceutical products of different dosage form. Oral route is considered most natural, uncomplicated, convenient and safe due to its ease of administration, patient acceptance and cost-effective manufacturing process. Gastroretentive drug delivery system was developed in pharmacy field and drug retention for a prolonged time has been achieved. The goal of this study was to formulate and in-vitro evaluate Ciprofloxacin HCl controlled release matrix floating tablets. Ciprofloxacin HCl floating matrix tablets were prepared by wet granulation method using two polymers such as HPMC K100M (hydrophilic polymer) and HPMC K15M. All the Evaluation parameters were within the acceptable limits. FTIR spectral analysis showed that there was no interaction between the drug and polymers. In-vitro dissolution study was carried out using USP dissolution test apparatus (paddle type) at 50 rpm. The test was carried out at 37 ± 0.5 0C in 900ml of the 0.1 N HCl buffer as the medium for eight hours. HPMC K100M shows a prolonged release when compared to HPMC K15M. These findings indicated that HPMC K100M can be used to develop novel gastroretentive controlled release drug delivery systems with the double advantage of controlled drug release at GIT pH. On comparing the major criteria in evaluation such as preformulation and in vitro drug release characteristics, the formulation F8 was selected as the best formulation, as it showed the drug content as 99±0.4% and swelling index ratio was 107.14, and in-vitro drug released 61.31±0.65% up to 8 hours. Results indicated that controlled Ciprofloxacin HCl release was directly proportional to the concentration of HPMC K100M and the release of drug followed non-Fickian diffusion. Based on all the above evaluation parameters it was concluded that the formulation batch F8 was found to be best formulation among the formulations F1 to F8 were prepared.

Analytical method development and validation for the estimation of Mirabegron in pure and its solid dosage form by UV spectrophotometric method

A simple, economical, rapid, accurate, precise spectrophotometric method has been developed and validated according to ICH Guidlines for the Mirabegron as active pharmaceutical ingredient (API) by UV spectrophotometric method. The absorption maxima of Mirabegron was found to be at 249 nm wavelength using 1N Hcl as a solvent. Linearity range was found to be 3-15μg/ml, with the correlation coefficient being more than 0.999. The relative standard deviation was found to be < 2%. The percentage recovery was within the range of 98% -105%, indicating that there is no significant interference from the other ingredients present in the formulation. The method can be applied for the routine analysis of Mirabegron as API in pharmaceutical preparation.

Formulate and evaluate once daily sustained release tablet of highly soluble drug of metformin HCL

The aim of the present study was to design an oral sustained release matrix tablet of highly water soluble biguanide anti diabetic drug. The matrix tablets are prepared by melt granulation method using HPMC K 200M as hydrophilic drug release retarding polymer, and stearic acid as melt able binder as well as hydrophobic carrier. The drug and excipients compatibility was studied by FT – IR. The formulated matrix tablets were characterized for physical parameters and in vitro dissolution profile. FT – IR spectra revealed the absence of drug excipients interaction. The physical parameters of the tablets were found within the limits. The drug release kinetics demonstrated that by increasing the concentration of hydrophilic polymer and hydrophobic carrier the drug release rate was retarded proportionally. Kinetic modelling of in vitro release profile revealing that the drug release from the matrix tablets following first order kinetics, and the drug release mechanism of optimized (F7) formula following non fickian transport mechanism. Accelerated stability studies were performed according to ICH guide lines. Temperature 40±20 c and relative humidity 75±5% RH to study physical and chemical changes of formulation. No physical or chemical changes were observed after t accelerated stability studies.

Formulation and evaluation of matrix tablets of Eperisone hydrochloride

The aim of the present research is to develop and optimize Eperisone Hydrochloride extended release matrix tablets. Eperisone Hydrochloride is an antispasmodic drug mainly used to relieve pains it acts by relaxing the skeletal and smooth vascular muscles by blocking spinal reflexes drug which has oral bioavailability of 70% due to hepatic metabolism. Sustained release matrix tablets of Eperisone Hydrochloride were prepared through wet granulation technique by using HPMC K4M and EC as polymers, PVPK30 as binder, Magnesium stearate as lubricant and Talc as glidant. The granules of different formulations were determined for pre compression parameters. The prepared granules along with the excipients were then compressed. The formulated tablets were evaluated for physical characteristics viz. Hardness, Thickness, % Weight variation, Friability and the drug content. Furthermore the tablets evaluated for the in vitro release studies. Out of all the 8 formulations F7 showed desired characteristics in the physical parameters and in vitro drug release of 85.48% in 12hrs.The F7 dissolution data was best fitted to the Zero order model. The prepared Eperisone Hydrochloride matrix tablets found to be having a potential extended drug release.

An overview on comparative study of registration requirements for generics in US, Canada and Europe

Generic Drug Product approval is most stringent and crucial process for company with different rules and regulation in different country. For the registration of the product company has to follow regulatory rules and requirement of country specific agency. Company should apply product marketing authorization as per norms of country requirements and should manage life cycle of that product throughout market. Need to understand and describe the various regulatory requirements for the generic drug approval process and comparison of regulated country. To understand the technical requirements required to market medicines in regulated pharmaceutical market. To evaluate similarities and differences within regulated market of U.S, Canada, and Europe. To understand and evaluate differences of post approval Changes within regulated market.

Formulation and evaluation of lansoprazole loaded enteric coated microspheres

The research focuses on the development of multiparticulate delivery system for acid-labile Lansoprazole to prevent its degradation in the acidic environment of the stomach and enhance its bioavailability via intestinal absorption. This problem can be solved by enteric coating. In this project, cellulose acetate phthalate a polymer usually utilized for gastrointestinal film coating of tablets, was used to prepare enteric microspheres of lansoprazole with solvent evaporation technique in various formulations such as F1, F2, F3, F4, F5 with drug: polymer ratios of 1:1, 1:2, 1:3, 1:4, 1:5 respectively. FTIR study indicated compatibility between drug and polymer. Increase in concentration of polymer increased spheriocity and mean diameter of the microspheres. The drug entrapment efficiency was in the range of 72.23% to 88.64%. SEM revealed that microspheres were found spherical and porous. In-vitro study proves that drug release slowly increases as the pH of the medium increased and prevents degradation of drug in acidic pH. In-vitro drug release was found to be 92.80%, 94.55%, 92.72%, 96.34%, 98.65% in all 5 formulations. All 5 formulations showed gastric resistance around 80-90%. So it is concluded that the developed enteric coated microspheres of Lansoprazole prevented drug release in the stomach which would lead to significant improvement in its bioavailability through enhanced intestinal absorption.

Erythrocyte as novel cellular drug delivery system

Nowadays so many carrier systems are used for delivery of drug or any other therapeutic agent to specific tissues or cells for achieving desired therapeutic efficacy. Using drug delivery systems can improve action of therapeutic agent and reduce their toxicity. As a novel approach the erythrocyte or red blood cells are used for drug delivery. The resealed erythrocyte is a cellular carrier have more advantage than other carrier system. Based on various studies found that erythrocyte have greater potential in delivery of biopharmaceuticals, therapeutically significant peptides and proteins, nucleic acid-based biological, antigens, anticancer drug and vaccines. The main problem obtain in case of existing carrier systems are biocompatibility of carrier and its degradation products. The biocompatibility, non-pathogenicity, non-immunogenicity and biodegradability make erythrocyte unique and useful carriers. They also possess longer circulation half-life and zero order drug release kinetics. Resealed erythrocyte carriers have certain impact among the activity of certain therapeutic agent like anti-inflammatory drugs, steroids, chemotherapeutic agents by reducing their side effect upon incorporation with these carriers. The general preparation step of resealed erythrocyte involve separation of erythrocyte from blood the organism of interest and using different methods the erythrocyte broken and the therapeutic agent or drug entrapped into the erythrocyte. This review article highlights the characteristics, isolation techniques of erythrocyte, preparation method, evaluation, application of resealed erythrocyte as carrier in drug delivery systems.

Development and characterization of miconazole nitrate transfersomal gel

Miconazole nitrate (MIC) is an antifungal drug used for the treatment of superficial fungal infections. However, it has low skin permeability. Hence, the basic idea behind the development of such a system, transfersomes is to maintain a sustain release of drug from the dosage form and for target delivery. Miconazole nitrate was formulated as transfersomes, half-life can be increased and the desired effect can be obtained. MIC transfersomes were prepared using a thin lipid film hydration technique. The prepared transfersomes were evaluated with respect to entrapment efficiency (EE%), particle size, and quantity of in vitro drug released to obtain an optimized formulation. The optimized formulation of MIC transfersomes was incorporated into a Carbapol 934 gel base which was for drug content, pH, spreadability, viscosity, in vitro permeation, and in vitro activity. The prepared MIC transfersomes had a high EE% ranging from 65.45% to 80.11%, with small particle sizes ranging from 368 nm to 931 nm. The in vitro release study suggested that there was an inverse relationship between EE% and in vitro release. In 24 hrs the drug release was observed ranging from 79.08% to 88.72%. The kinetic analysis of all release profiles was found to follow Higuchi’s diffusion model. All independent variables had a significant effect on the dependent variables (p-values < 0.05). Therefore, Miconazole nitrate in the form of transfersomes has the ability to penetrate the skin, overcoming the stratum corneum barrier. When the data subjected to zero order and first order kinetics model, a linear relationship was observed with high R2 values for zero order model as compared to first order model and suggested that the formulations followed zero order sustained release.