Current Issue : July - September Volume : 2011 Issue Number : 3 Articles : 10 Articles
Pharmaceutical inventions are increasingly focusing on delivery systems which enhance desirable therapeutic objectives while minimizing side effects. Recent trends indicate that multiparticulate drug delivery systems are especially suitable for achieving sustained release with low risk of dose dumping. In present investigation hollow microspheres (Microbaloons) were developed as a dosage form. Microballoons were prepared by the emulsion solvent diffusion method using ethyl cellulose with drug in a mixture of dichloromethane and ethanol. Preliminary studies revealed that the concentration of polymer and stirring speed significantly affected the characteristics of microballoons. It was found that temperature is an important factor which determined the formation of cavity inside the microspheres. The effect of process variables such as: polymer concentration and stirring rate were evaluated on the yield, particle size, Entrapment efficacy, floating behaviors and drug release of microspheres using a 32 factorial design. The optimum batch of microsphere exhibited good flow property, sustained drug release, remained buoyant for more than 8 hrs, entrapment efficiency up to 76 %w/w. SEM confirmed the hollow structure of microsphere. The results of 32 full factorial design revealed that the concentration of ethylcellulose (X1) and stirring speed (X2) significantly affected drug entrapment efficiency, percentage release after 8 h and particle size of microspheres....
Earlier liposomes were known as the lipid vesicles which deliver drugs to outer layers of skin. Now-a-days, Ethosomes are very popular which penetrate through stratum corneum and deliver drug to the deeper layers of skin. Ethosomes offer non invasive delivery of any sized drug molecule whether that is hydrophilic or lipophilic. The formulation and evaluation of ethosomes of ketoconazole was carried out in this study. Ethosomes contain phospholipid (1-3%), ethanol (20-40%), propylene glycol (10%) and distilled water. Ethosomes were prepared by “cold” method and characterized for vesicular size, shape, DSC, Entrapment efficiency, X-RD, in vitro skin diffusion study, skin irritation study and stability study. Optical microscopy, Scanning Electron Microscopy and Malvern Size analyser showed that ethosomes were spherical, unilamellar, nanometric size, low polydispersity index (Less than 0.3) vesicles. Sonicated ethosomes had smaller size (248 ± 12.6 nm) and were uniform in shape than unsonicated ethosomes (681 ± 22.6 nm). Entrapment efficiency percentage of best formulation was 62.11 ± 2.11%. In vitro skin diffusion study showed 78.61 ± 1.03 % drug diffused in 12 h. Skin irritation study showed no remarkable irritation. Stability study at 4 ± 2°C and at Room Temp. for 60 days showed minor increase in vesicle size....
Zolpidem Tartrate is a non-benzodiazepine, sedative-hypnotic, majorly used in various types of insomnia. Usual dosage regimen is 5mg, 2 times a day or 10mg, once daily having t1/2 2.5 hrs, undergoes hepatic first pass metabolism. Therefore in present study attempt has been done to formulate and evaluate the fast dissolving sublingual tablet of Zolpidem Tartrate. Tablets were prepared by wet granulation method using superdisintegrants, Sodium starch glycolate and Cross-povidone. Camphor was added in the formulation as a sublimating agent. The tablets were evaluated for weight variation, hardness, friability, wetting time, water absorption ratio, and disintegration time and dissolution study. Among studied formations hardness was found in 3-3.5 kg/cm2 range and friability less than 1%.Weight variation taste complies with pharmacopoeias limits. Sublimation of Camphor from tablets resulted in better tablets as compared to the tablets prepared from granules that were exposing to vacuum. The systematic formulation approach helped in understanding the effect of formulation processing variables....
A gastro retentive floating drug delivery system with multiple-unit minitab’s based on gas formation technique was developed in order to prolong the gastric residence time and to increase the overall bioavailability of the drug. The system consists of the drug-containing core units prepared by direct compression process, which are coated with three successive layers of an inner seal coat, effervescent layer (sodium bicarbonate) and an outer gas-entrapped polymeric membrane of an polymethacrylates (Eudragit RL30D, RS30D, and combinations of them). Only the system using Eudragit RL30D and combination of them as a gas-entrapped polymeric membrane could float. The time to float decreased as amount of the effervescent agent increased and coating level of gas-entrapped polymeric membrane decreased. The optimum system floated completely within 3 min and maintained the buoyancy over a period of 12 h. The drug release was controlled and linear with the square root of time. Increasing coating level of gas-entrapped polymeric membrane decreased the drug release. Both the rapid floating and the controlled release properties were achieved in the multiple-unit floating drug delivery system developed in this present study. The analysis of the parameter dissolution data after storage at 40°C and 75% RH for 3 months showed, no significant change indicating the two dissolution profiles were considered to be similar (f2 value is more than 50)....
Intranasal Therapy has been an accepted form of treatment in the Ayurvedic system of Indian Medicine. The interest in intranasal delivery of drugs as a non-invasive is increased.Nasal delivery is a feasible alternative to oral or parenteral administration for some drugs because of the high permeability of the nasal epithelium, rapid drug absorption across this membrane and avoidance of hepatic first-pass metabolism. Besides this, intranasal route has also been successfully exploited for bypassing the blood brain barrier and subsequently delivering drug molecules to central nervous system. The present article highlights the advantages, barriers, physicochemical factors and formulation related parameters affecting the nasal drug delivery. Also, the applications of nasal route for delivery of peptides and proteins, non-peptide drugs, vaccines and drug molecules to CNS have been summarized in depth....
The objective of the present study was to develop once-daily sustained-release matrix tablet of fluvastatin, an antihyperlipidemic drug. The tablets were prepared by the dry granulation method. The tablets were evaluated for various physicochemical parameters, in-vitro drug release, swelling and erosion studies and stability. At lower polymer concentration, the erosion front movement was found to be more than diffusion front and drug release was anomalous as compared to zero order kinetics at higher concentration. The HPMC: HPC and MCC based test formulation (HM4) was expected to compete with the reference standard for bioequivalence and bioavailability. An extended release hydrophilic matrix tablet of a water soluble drug fluvastatin was prepared successfully by dry granulation method....
Solid lipid nanoparticles (SLN) loaded with highly hydrophilic drug, rosiglitazone maleate were prepared by cold homogenization technique. Glyceryl monostearate was used as lipid core and lecithin E-80 as the shell material. Both lipid and drug were dissolved using dimethyl sulfoxide (DMSO). Oleic acid was also employed as surfactant. The physiochemical properties of SLNs with various lipid composition, drug content and altered homogenizing time were optimized to obtain high quality nanoparticles. The enhancement of lecithin content in lipid matrix resulted in smaller particle of SLNs. The mean particle size measured by photon correlation spectroscopy (PCS) was ranged from 140.2-467.6 nm. The drug entrapment efficiency (EE) and drug loading capacity (DL) were determined using fluorescence spectroscopy, were reach up to 81.2 ± 2.5% and 7.1±0.23% respectively. The drug release behavior was studied by using dialysis bag method. The study of drug release showed that the drug release could last up to 48 h, and the rate was delayed by the addition of lecithin and/or oleic acid in the formulations. The physical stability experiment showed that the SLNs were stable for 2 months under room temperature. Moreover, the cellular cytotoxicity of rosiglitazone maleate against cell could be improved by the entrapment of SLNs. In conclusion, SLN with small particle size, high EE and relatively high DL capacity for rosiglitazone maleate can be obtained by this method....
In the present work a gold modified pencil graphite electrode (GPGE) was used for the determination of insulin present in the pharmaceutical sample. Cresol, an electroactive phenolic compound present in insulin pharmaceutical sample which interfere for the detection of insulin. In this paper, the removal of cresol from dialysis process, than obtained solution was freeze dried, followed by detection of insulin by electrophoresis and differential pulse voltammetric (DPV) studies were achieved. The proposed method was applied for the determination of insulin in pharmaceutical sample....
As the role of monocytes and macrophages in a range of diseases is better understood, strategies to target these cell types are of growing importance both scientifically and therapeutically. As particulate carriers, liposomes naturally target cells of the mononuclear phagocytic system (MPS), particularly macrophages. Loading drugs into liposomes can therefore offer an efficient means of drug targeting to MPS cells. Physicochemical properties including size, charge and lipid composition can have a very significant effect on the efficiency with which liposomes target MPS cells. MPS cells express a range of receptors including scavenger receptors, integrins, mannose receptors and Fc-receptors that can be targeted by the addition of ligands to liposome surfaces. These ligands include peptides, antibodies and lectins and have the advantages of increasing target specificity and avoiding the need for cationic lipids to trigger intracellular delivery. The goal for targeting monocytes/macrophages using liposomes includes not only drug delivery but also potentially a role in cell ablation and cell activation for the treatment of conditions including cancer, atherosclerosis, HIV, and chronic inflammation....
Thermosensitive nanocarriers as the ââ?¬Å?smartââ?¬Â drug delivery systems have shown tremendous promise in the field of controlled drug delivery due to their special property. Thermosensitive nanocarriers with long circulation properties can accumulate in the pathological sites by enhanced permeability and retention (EPR) effect or attach targeting ligands to the surface of the nanocarriers, and the drug release rates of these pharmaceutical nanocarriers can be adjusted in response to thermal variability of the environment. In this paper, we first discuss the classification of thermosensitive polymer according to their functional properties in thermosensitive nanocarriers. On the basis of this, our main purposes are focused on reviewing the characteristics of various thermosensitive nanocarriers including the strategies for their functionalization, thermosensitive behavior, or site-specific targeting. Furthermore, the paper discusses the current and future trends of the thermosensitive nanocarriers in controlled drug delivery....
Loading....