The aim of the present study is to develop transdermal patch loaded with proniosomes that is capable of delivering the entrapped drug over an extended period of time. Metformin HCl, a hydrophilic drug used for the treatment of type 2 diabetes mellitus. Metformin HCl has short half life of 4-6 hrs with oral bioavailability of about 50-60%. Proniosomal TDDS can overcome the permeation barrier of the skin and enhance the permeation of therapeutically active drug molecule. Metformin hydrochloride proniosomes was prepared by coacervation phase separation method using span 40, span 60, cholesterol and soya lecithin. In this study 6 formulations of proniosomes were prepared and their characteristics such as physical appearance, pH, viscosity, particle size, zeta potential, encapsulation efficiency, surface morphology, drug content and in-vitro drug release studies were investigated. FT-IR study confirmed the drug-polymer compatibility. Particle size of proniosome was obtained in nanometers. Zeta potential of formulation was found negative indicating the stability of the proniosome. F2 showed higher encapsulation efficiency (87.08 ±0.35) and % CDR (64.22%). Proniosomal formulation F2 was selected and converted into transdermal patches using PVA as backing membrane, HPMC E50 and PVP k30 as rate controlling membrane. Evaluation studies like thickness, weight uniformity, folding endurance, % moisture content, drug content and in vitro drug release studies were carried out. The formulation FPT2 showed higher drug content of 17.14 ± 0.32 mg and maximum drug release of 60.58% in 8 hrs. From the data obtained in this study, it was concluded that transdermal patch loaded with proniosomes of Metformin HCl are promising for sustained drug delivery.
Liposomes are the biocompatible and stable can be crafted to carry both water and fat-soluble nutrients. If the formulate are correctly, and they can facilitate the absorption as soon as they land on the tongue, and they can help to protect the breakdown by the digestive acids and enzymes. Liposomes are the nanocarriers comprised of lipid bilayers encapsulating an aqueous core. Liposomes are the complex defence systems which protects itself, liposomes shows the predominant interaction of cells with either simple adsorption or subsequent endocytosis. The Liposomes containing drugs or a variety of elements and their utilisation as a form, tool, or reagent in the fundamental studies of cell interfaces. The ability of Liposomes to encapsulate a wide variety of diagnostic and therapeutic agents has led to significant interest in utilising Liposomes as nanocarriers for theranostic application. This review presents an overview of the various aspects of the Liposomes with special emphasis on nanocarriers based on strategies.
Pathloth Sony*, A. V. S. Rajeswari, J. V. C. Sharma, A. V. S. S. S. Gupta.
The objective of the present work is to design and development of floating in situ gel containing Ibuprofen in order to achieve an extended retention in the upper GIT, which may enhance the absorption and thereby improved bioavailability. Floating in situ gel of Ibuprofen were prepared by ionic gelation method using Sodium Alginate, Gellan Gum, HPMC K 4M. The prepared in situ gel were evaluated for various parameters like physical appearance, in vitro gelation study, viscosity, in vitro floating study, drug content, water uptake by the gel, density, gel strength, in vitro drug release study, in vitro drug release kinetics and stability study. FT-IR study confirmed the drug-polymer compatibility. All Floating in situ gel formulations showed optimum pH in the range of 7.53 - 7.64 and optimum density of less than ̴ 1.004g/cm3. Among all formulations, F3 (0.2% of Gellan gum) and F6 (0.2 % of HPMC K4M) showed shorter floating lag time and longer total floating time and also drug release rate (75.59% in 8hrs and 76.79% in 8hrs), hence it is considered as the best formulation. The data obtained in this study thus suggests that the floating in situ gel of Ibuprofen are promising for sustained drug delivery which can be used for reducing dosing frequency.
The success of formulation depends on how capably it makes the drug available at the site of action. Therapeutic effectiveness of a drug depends upon the bioavailability which ultimately depends upon the solubility of drug molecules in case of oral formulations. So, solubility enhancing techniques like co-solvency, hydrotropy, co-crystallisation, salt formation, change in pH, addition of solubilizing agent, micronization, complexation, modification of crystal habit, solid dispersion have to be used to enhance solubility of poorly soluble drugs. The intention of this article is to describe the solubilisation techniques for improving bioavailability of poorly soluble drugs.
B. Hemalatha*, K. Manasa, P. Kavya, T. Pavani Priya, K. Padmalatha.
Scattered polymer nanocapsules can fill in as nano-sized medication transporters to accomplish controlled delivery just as productive medication focusing on. The scattering soundness and the essential physiological reaction are for the most part dictated by the kind of the surfactant and the idea of the external covering. Their delivery and debasement properties generally rely upon the synthesis and the design of the case dividers. Another significant standard is the container size, where an ideal is for the most part seen for radii going somewhere in the range of 100 and 500nm. Nanocapsules can be set up by four essentially various methodologies: interfacial polymerization, interfacial precipitation, interfacial testimony and self get-together systems. Every one of these methods offer their individual focal points and burdens with regards to the plan of streamlined medication transporter frameworks. The main case boundaries, for example, container span appropriation, the case surface, the thickness and the porousness of the case layer and its warm or substance deterioration, are talked about and models are appeared. In mix with effective readiness systems, nanocapsule scatterings take into account new and promising methodologies in numerous sorts of drug treatments.
J. Laxapathi*, P. Sony, A. V. S. Rajeswari, J. V. C Sharma, A. V. S. S. S. Gupta.
The aim of the work was an attempt to make the formulation of mouth dissolving tablets by producing Pores in tablets by Sublimation technique, using subliming agents. Drug-carrier complex were prepared by solid dispersion solvent evaporation method of 1:3 ratio (Drug: carrier). Mouth Dissolving tablets of Sertraline HCl were punched by direct compression method. The compressed tablets are subjected to the process of sublimation in Hot air oven. All the formulated tablets were subjected for formulation evaluation parameters. From the FTIR studies, the drug-polymers compatibilities were confirmed. In-vitro drug release studies the hardness of the tablet was in the range of 2.5-3.0kg/cm2. % friability of the tablet was less than 1. In-vitro dispersion time for tablets was in between 26- 47sec. in-vitro drug release studies were carried out for a period of 8min, results showed that more than 90% of the drug was released from all the batches. Among the all six formulations, the formulation containing 5mg of camphor and 5mg of croscarmellose sodium (F2) showed highest drug release in short time. For this study we can make conclude that the developed novel method for preparing MDTs of Sertraline HCl increases the porosity and enhances the bioavailability.
Sachinkumar Bhairagond*, K. C. Viresh, A. R. Shabaraya.
Doxorubicin is a widely used anti-cancer drug which also has a comparatively good therapeutic effect against Rheumatoid Arthritis. This study shows a newer approach to treatment of Rheumatoid Arthritis with Doxorubicin using an transdermal formulation for Doxorubicin with easily available polymers like Hydroxy propyl methyl cellulose, Sodium alginate, Polyethylene Glycol etc using solvent casting technique and conduct in-vitro evaluation tests to prove the stability and efficacy of the same.
Barish*, E. Abrahm Theodore, M. Raj Kumar, M. Mumtaj Begum, S. Princy.
The main objective of the present work was to formulate and evaluate Doxorubicin hydrochloride microspheres using polymers like HPMC and starch which will prolong the drug release leading to minimize the peak and valley effect in the plasma and provides patient convenience to perform the pre-formulation studies like Calibration curve of Doxorubicin hydro chloride and FIIR of Doxorubicin hydrochloride HPMC and starch to formulate a sustained release drug delivery of Doxorubicin microspheres containing 250mg of drug with polymers starch (Formula FS) and HPMC (Formula FH) respectively by Solvent evaporation method. Evaluation of microspheres to evaluate the post formulation parameters like appearance, solubility, SEM % yield, % entrapment efficiency, in vitro drug release, release kinetics and stability studies. The newly prepared microspheres were evaluated for morphology, vesicle size determination, percentage of drug encapsulation, drug leakage studies from vesicles, osmotic shock and in vitro release profile and came to conclusions to the point that microsphere enhances the therapeutic effectiveness of Doxorubicin producing prolonged activity and simultaneously minimizing the side effects.
Barish*, E. Abraham Theodore, S. Princy, M. Mumtaj Begum, S. Aiswarya.
The present study was aimed to formulate orodispersible tablets of atorvastatin by using superdisintegrants in order to enhance the bioavailability. The orodispersible tablets displaying faster disintegration providing significant advantages over traditional dosage forms. The tablets are prepared by direct compression technique by using superdisintegrants like sodium starch glycolate and cross caramellose sodium. Formulations F1 to F8 were made with varying proportions of superdisintegrants. The drugs excipients compatibility studies were performed by FTIR and DSC indicates there is no compatibility issue. All the prepared formulations passed quality control test for tablets. The in vitro dissolution rate of all the formulations shows improved dissolution rate. The F8 formulation shows high dissolution rate compared to other formulations. The prepared formulations significantly enhancing the solubility and dissolution rate of the drug.
The present research study was aimed to formulate, evaluate and optimize temozolomide solid lipid nanoparticles by central composite design for treatment of Glioblastoma multiforme. The temozolomide solid lipid nanoparticles were prepared by solvent injection method using palmitic acid as lipid and tween 80 as surfactant. The independent variables used in the formulation were surfactant concentration (X1) and drug: lipid (X2), their effects were observed with regard to dependent variables like % entrapment efficiency (R1) and % drug release (R2). Total 13 formulations were prepared and evaluated. The Differential scanning calorimetry and Fourier transform infrared studies indicated compatibility between drug and excipients. All temozolomide solid lipid nanoparticle formulations showed sizes in nanometre range, with high % entrapment efficiency and prolonged drug release up to 24 hours. The optimized formulation showed an entrapment efficiency of 85.65% and 95.343 ± 0.88% drug release for an extended period of 24 hours. Scanning electron microscopic studies revealed discrete spherical shape of temozolomide solid lipid nanoparticles. This study indicates that solid lipid nanoparticles could be a feasible carrier for temozolomide delivery to brain for treatment of glioblastoma multiforme. However further studies are required to endorse their potential as an effective drug delivery system.
Shaik Abdul Razak*, K. Arshad Ahmed Khan, N. Vijaya Bhaskar, P. Ravi Prakash.