Formulation and Characterization of Aceclofenac -Aloe vera Transemulgel.

The present research was aimed to formulate aceclofenac transemulgel using Aloe vera as gel base. The prepared formulations were subjected to physical characterization, in-vitro and in-vivo assessment. Aceclofenac, a hydrophobic potential non steroidal anti inflammatory drug, causes ulceration upon chronic oral administration, could be formulated into transemulgel to enhance therapeutic efficacy and to lower the unwanted side effects. The transemulgel was prepared from aqueous Aloe vera gel and aceclofenac emulsion. The prepared transemulgel was evaluated for its pH, viscosity, drug content, skin irritation, in-vitro diffusion and accelerated stability studies. The prepared aceclofenac-Aloe vera tranemulgel and commercial aceclofenac gel were subjected to pharmacodynamic studies in albino rats of Wistar strain employing carrageenan induced left hind paw edema method to assess the anti-inflammatory effect. The transemulgel showed a pH of 6.78 and viscosity of 18 cps. In-vitro diffusion data revealed better permeation characteristics. Topical application of formulation found no skin irritation. Stability study has proved the integrity of the formulation. The prepared aceclofenac Aloe vera transemulgel showed better in-vitro drug release when compared with the commercial aceclofenac gel formulation. Anti-inflammatory activity in treated rats showed the significant paw volume reduction at p<0.05 compared with that of control. Thus, it is concluded that aceclofenac, a potential non steroidal anti inflammatory drug, showed high therapeutic efficiency when formulated into transemulgel using aqueous Aloe vera as gel base.

Effect of Argemone mexicana (L.) against lithium-pilocarpine induced status epilepticus and oxidative stress in Wistar rats.

Argemone mexicana (L.) has a role in the treatment of epileptic disorders in Indian traditional system of medicine. We studied its effect on induced status epilepticus (SE) and oxidative stress in rats. SE was induced in male albino rats by administration of pilocarpine (30 mg/kg, ip) 24 h after injection of lithium chloride (3 mEq/kg, ip). Different doses of the ethanol extract of A. mexicana were administered orally 1 h before the injection of pilocarpine. The severity of SE was observed and recorded every 15 min for 90 min and thereafter at every 30 min for another 90 min, using the Racine scoring system. In vivo lipid peroxidation of rat brain tissue was measured utilizing thiobarbiturate-reactive substances. Both in vitro free radical nitric oxide and 2,2-diphenyl-1-picryl hydrazyl scavenging activities of the extract were also determined. The SE severity was significantly reduced following oral administration of the extract at 250, 500 and 1000 mg/kg doses. None of the animals from groups 3 to 5 (with A. mexicana extract) have exhibited forelimb clonus of stage 4 seizure. The extract also exhibited both in vivo and in vitro antioxidant activities.

Solid self microemulsification of Atorvastatin using hydrophilic carriers: a design.

CONTEXT: Atorvastatin has a limited advantage to formulate oral dosage forms. OBJECTIVE: To enhance the solubility of Atorvastatin and to design the suitable solid self-microemulsifying drug delivery systems (S-SMEDDS) Materials and methods: The clear and transparent self-microemulsifying drug delivery system (SMEDDS) were formulated using coconut oil and isopropyl myristate as lipid phases; Tween 80 as surfactant; PEG 400 and glycerin as co-surfactant at 2:1, 3:1, 1:2 and 1:3 ratio. The pseudo ternary phase diagrams were constructed to identify the microemulsion region. The SMEDDS were evaluated for zeta potential, poly dispersity index, globule size, pH, viscosity and drug release. The solid SMEDDS were developed by employing adsorption and melt granulation methods. The S-SMEDDS were evaluated for micromeritics, morphology, solid state property, reconstitution ability, drug release and stability. RESULTS: The micro formulations formed with particle size of 25 nm had shown a 3-folds rise in drug release. The solid SMEDDS had reconstituted to a good microemulsion rapidly in 1-3 min, with a release of 94.62% at the end of 30 min and behaved as immediate releasing capsules. Their shelf-life was found to be 1.3 years. DISCUSSION: The 1:3 ratio SMEDDS had shown more drug release owing to their less particle size. The solid SMEDDS had shown an increased dissolution profiles than atorvastatin. The solid state of the drug had changed in formulation inferring their enhanced solubility. CONCLUSION: The solid form of atorvastatin liquid SMEDDS had been formulated successfully with enhanced shelf life and solubility.

Formulation and pharmacodynamic evaluation of glibenclamide incorporated niosomal gel.

OBJECTIVE: The research aims to formulate and develop the controlled release profile of glibenclamide by encapsulating glibenclamide into niosomes followed by incorporation into an aqueous gel base. MATERIALS AND METHODS: Glibenclamide incorporated niosomes were prepared by a modified ether injection technique using Span 20/Span 80 and cholesterol. The prepared niosomes were evaluated for chemical incompatibility by FT-IR, morphology, vesicle dimension, encapsulation efficiency, in-vitro diffusion and drug release kinetics. Niosomal gels were prepared by incorporating the optimized niosomes into a gel base containing Carbopol 934 and evaluated for viscosity, in-vitro diffusion and in-vivo pharmacodynamic activity. RESULTS AND DISCUSSION: The results indicated that relationship between the amount of Span and niosomal vesicular diameter was inversely proportional. Microscopic images have illustrated the sphere shape vesicles. The cumulative percentage of drug release from niosomal suspension was observed in the order GN-4>GN-2>GN- 6>GN-5>GN-3>GN-1. Glibenclamide gel showed highest percentage drug release when compared to niosomal gel. Invivo study revealed that the glibenclamide incorporated niosomal gel formulation; GNG-1 is more efficient in lowering blood glucose levels in experimental animals. CONCLUSION: The niosomal gel of glibenclamide had released the drug in well controlled manner which is supported by pharmacodynamic activity with evidence of consistent lowering of blood glucose levels.

An overview on in situ micronization technique - An emerging novel concept in advanced drug delivery.

The use of drug powders containing micronized drug particles has been increasing in several pharmaceutical dosage forms to overcome the dissolution and bioavailability problems. Most of the newly developed drugs are poorly water soluble which limits dissolution rate and bioavailability. The dissolution rate can be enhanced by micronization of the drug particles. The properties of the micronized drug substance such as particle size, size distribution, shape, surface properties, and agglomeration behaviour and powder flow are affected by the type of micronization technique used. Mechanical communition, spray drying and supercritical fluid (SCF) technology are the most commonly employed techniques for production of micronized drug particles but the characteristics of the resulting drug product cannot be controlled using these techniques. Hence, a newer technique called in situ micronization is developed in order to overcome the limitations associated with the other techniques. This review summarizes the existing knowledge on in situ micronization techniques. The properties of the resulting drug substance obtained by in situ micronization were also compared.

Transmucosal delivery of metformin- a comprehensive study.

Discovered in the 1920s, the biguanide metformin hydrochloride is still the first line drug in the management of Type 2 diabetes mellitus. Metformin hydrochloride is absorbed slowly and incompletely from the gastrointestinal tract. The present research work was undertaken with the aim of developing a fast dissolving film of metformin hydrochloride, suitable for oral trans mucosal administration. Fast dissolving films allow rapid drug dissolution in the oral cavity, ensuring bypass of first pass metabolism resulting in rapid absorption. Films of metformin were prepared by solvent casting method using Hydroxypropyl methylcellulose K15 (HPMC). Six formulations (F1-F6) of metformin hydrochloride were prepared and evaluated for their physical characteristics such as tackiness, thickness, tensile strength, elongation, weight variation, folding endurance, drug content and surface pH. The compatibility of the drug with HPMC was confirmed by FTIR studies. The formulations were subjected to disintegration, in-vitro drug release and the optimised formulation was evaluated for pharmacodynamic studies in diabetic rats. Among the formulations (F1-F6) F4 was found to be the best formulation which contained Hydroxypropyl methyl cellulose K15 at weight ratios of 1:4 and showed excellent film forming characteristics such as disintegration time at 42 sec and percentage drug release of 94.2% within 5 minutes. Pharmacodynamic assessment in diabetes induced rats demonstrated that the fast dissolving films of metformin had a quicker onset of action compared to conventional formulation.

In-vitro assessment and pharmacodynamics of nimesulide incorporated Aloe vera transemulgel.

The aim of the investigation was to prepare nimesulide emulsion for incorporation in Aloe vera gel base to formulate 'nimesulide - Aloe vera transemulgel' (NAE) and to carryout in-vitro assessment and in-vivo anti-inflammatory studies of the product. Although the use of nimesulide is banned for oral administration, due to its potential for inducing hepatotoxicity and thrombocytopenia, the use of nimesulide for topical delivery is prominent in the treatment of many inflammatory conditions including rheumatoid arthritis. The drug loading capacity of transdermal gels is low for hydrophobic drugs such as nimesulide. Nimesulide can be effectively incorporated into emulgels (a combination of emulsion and gel). Aloe vera has a mild anti-inflammatory effect and in the present study Aloe vera gel was formulated and used as a gel base to prepare NAE. The emulgels thus prepared were evaluated for viscosity, pH, in-vitro permeation, stability and skin irritation test. In-vivo anti-inflammatory studies were performed using carrageenan induced hind paw edema method in Wistar rats. The results were compared with that of commercial nimesulide gel (CNG). From the in-vitro studies, effective permeation of nimesulide from NAE (53.04 %) was observed compared to CNG (44.72 %) at 30 min indicating better drug release from NAE. Topical application of the emulgel found no skin irritation. Stability studies proved the integrity of the formulation. The percentage of inhibition of edema was highest for the prepared NAE (67.4 % inhibition after 240 min) compared to CNG (59.6 %). From our results, it was concluded that the Aloe vera gel acts as an effective gel base to prepare nimesulide emulgel with high drug loading capacity (86.4 % drug content) compared to CNG (70.5 % drug content) with significant anti-inflammatory effect.