Synthesis of some new 1,3,5-trisubstituted pyrazoles as antioxidant and antiinflammatory agents

A series of some new 1,3,5-trisubstituted pyrazoles was synthesized by the reaction of α-β dibromochalcones with phenylhydrazine hydrochloride. α-β-Dibromochalcones were prepared by the regioselective bromination of respective chalcones with tetrabutylammonium tribromide. The synthesized trisubstituted pyrazoles were evaluated for their anti-inflammatory and antioxidant properties. Keywords: α-β-Dibromochalcones, 1,3,5-Trisubstituted pyrazoles, Tetrabutylammonium tribromide, Anti-inflammatory and antioxidant activitie

A Review on Microsponge Delivery System

Microsponge is recent novel technique for control release and target specific drug delivery system. Microsponge technology has been introduced in pharmaceutical industry to provide the controlled release of active drug ingredient for the application into the skin in order to decrease systemic exposure and reduce local cutaneous reactions to active drugs. Microsponges comprises of microporous beads, typically 10-25 microns in diameter, loaded with active agent. The microsponge releases its active ingredient on a time mode, when applied to the skin,  and also in response to other stimuli that are used mostly for topical and recently for oral administration. Microsponge technology has many favourable characteristics which make It all around suitable as drug delivery vehicle. Microsponge systems can suspend or entrap a wide variety of substances, and then be incorporated into a formulated product such as a gel, cream, liquid or powder. The outer surface is mostly porous, allowing the sustained flow of substances out of the sphere. Microsponge drug delivery system causes increased efficacy for the topically active agents with enhanced safety and product stability for a longer period of time with reduction in side effects. In addition their non-allergenic, non-irritating, non-mutagenic and nontoxic behaviour makes them the suitable dosage form. The present review emphasis Microsponge drug delivery system along with its release mechanism. Keywords: Novel drug delivery system, Microsponges, Microsponge drug delivery system, Quasi-emulsion solvent diffusion method

Formulation and Evaluation of Fluconazole Microsponge using Eudragit L 100 by Quasi Emulsion Solvent Diffusion Method

The aim of the present study is to formulate and evaluate the fluconazole microsponge by using Eudragit L 100. Microsponge was made because they provide controlled as well as target specific release of the drug. Thus study the effect of stirring rate on the formation of microsponge. Microsponge containing Fluconazole were prepared by quasi-emulsion solvent diffusion method at different stirring rate i.e 500, 800, 1000, 1200 and 1500 rpm. Particle size of prepared microsponge was observed in the range of 76.2 to 32.5μm. Scanning electron microscopy revealed the porous, spherical nature of the microsponges. The production yield, entrapment efficiency and drug content were found to be 78.24%, 82.76%, 81.36%. The impact of Drug: Polymer ratio and process variables i.e stirring speed and stirring time on the physical features of microsponges like production yield, mean particle size, entrapment efficiency were examined. It was shown that production yield, drug content and entrapment efficiency was found to be increase with increase in drug polymer ratio while drug: polymer ratio has reverse effect on particle size, as drug: polymer ratio increase, particle size decrease. As the polymer concentration increased, more amount of polymer surrounding the drug, thus increasing the thickness of the wall of the polymer matrix which lead to extended diffusion path and ultimately to lesser drug release or more sustained release. The effect of stirring rate on the morphology of microsponge. The formulation with higher drug to polymer ratio 1:8 (i.e F4) was chosen to investigate the effect of stirring rate on the morphology of microsponges. The dispersion of the drug and polymer within the aqueous phase was found to be dependent on the agitation speed. As the speed was increased the size of microsponges was reduced and the microsponges were found to be spherical and uniform. Keywords: Novel drug delivery system, Microsponges, Eudragit L 100, Fluconazole, Quasi-emulsion solvent diffusion method

Preparation and Characterization of Itraconazole Microsponges using Eudragit RSPO and Study the Effect of Stirring on the Formation of Microsponges

The purpose of the present study was to prepare and evaluate Itraconazole loaded microsponges using Eudragit for the controlled release of the drug and study the effect of stirring rate on the formation of microsponges. Microsponges containing Itraconazole were prepared by using quasi-emulsion solvent diffusion method at different stirring rate i.e. 500, 800, 1000, 1200 and 1500rpm.  Particle size of prepared microsponge was observed in the range of 78.43 to 23.18 µm. Scanning electron microscopy revealed the porous, spherical nature of the microsponges. The production yield, entrapment efficiency, and drug content were found to be 80.88%, 84.53% and 82.89%. The formulation with higher drug to polymer ratio 1:10 (i.e. F5) was chosen to investigate the effect of stirring rate on the morphology of microsponges. As the speed was increased, the particle size of microsponges was reduced and uniform spherical microsponges were formed. As drug polymer ratio increased, Production yield, drug content and entrapment efficiency was found to be increased while drug: polymer ratio has reverse effect on particle size, as drug: polymer ratio increase, particle size decreases. The cumulative percentage drug release upto 8hrs for F5 was 89.54% and the mechanism of drug release from the formulations during the dissolution was determined using the zero order, first order, higuchi equation and Peppas equation. All formulations were best fitted to Zero order and peppas plot. The best formulation F5 follows Zero order release. Keywords: Microsponges, Itraconazole, stirring rate, Quasi-emulsion solvent diffusion metho

Advancement in Novel Drug Delivery System: Niosomes

Niosomes represent a promising drug delivery module. Noisome same as to liposome and Noisome represent alternative vesicular drug delivery systems with respect to liposomes, due to the noisome ability to encapsulate the different type of drugs within their multi environmental structure. Niosomes are thoughts to be a better system for drug delivery as compared to liposomes due to various factors like cost, stability etc. They are many types of drug deliveries that can be possible using niosomes like targeting, ophthalmic, topical, parenteral, etc. In recent research, comprehensive research carried over noisome as a drug carrier. Various drugs are enlisted and tried in noisome surfactant vesicles. Niosomes proved to better drug carrier system and has the potential to reduce the side effects of drugs and increased therapeutic effectiveness in various diseases. Noisome used more than fifty drugs are tried in niosomal formulations by the intravenous route, per oral administration, trans-dermal route of administration, and inhalation preparation, ocular nasal route of administration. Treatment of infectious diseases and immunization has undergone a revolutionary work in recent years. The large numbers of disease-specific biological have been developed, and also emphasis has been made to effectively deliver these biological. Niosomes shows an emerging class of novel vesicular systems. Niosomes are self-assembled vesicles composed primarily of synthetic surfactant and cholesterol. Comprehensive research carried over noisome as a drug carrier. Various drugs are enlisted and tried in noisome surfactant vesicles. This article presents an overview of the techniques of preparation of noisome, types of noisome, characterization and their applications. Keywords-Niosomes; Method of preparation; Evaluation study; Application of Niosome

Formulation and Evalution of Levamisole Niosomes by using Sonication method

Niosomes or non- ionic surfactants vesicles are one of the many different carriers for transporting a drug molecule to its site of action. Niosomes are vesicular system similar to liposomes that can be used for amphiphilic and lipophilic drugs. Niosomes are biocompatible, biodegradable, non- immunogenic and exhibit flexibility. Niosomes has been widely used for controlled release drug delivery system. Niosomes can entrap both hydrophobic and hydrophilic drugs.  Niosomes are chemically stable drug delivery systems. Niosomes are biocompatible, biodegradable, non- immunogenic and exhibit flexibility in structure. Niosomes have been widely used for controlled drug delivery system. They have been prepared with different ratios of surfactants and cholesterol and their properties have been determined by scanning electron microscopy. There are five batches of Levamisole niosomal preparations were prepared by changing the surfactant concentration but keeping the cholesterol concentration constant. The surfactant used Span40 and the five batches of niosomal preparations in the ratios of 1:1:1, 1:2:1, 1:3:1, 1:4:1 and 1:5:1 (Surfactant: cholesterol: drug). Furthermore, the release profiles, entrapment efficiency, size distribution and stability of these niosomes under various temperatures were studied. Niosomes were prepared using Span40 by using sonication method. The test changes in the characteristics of the liposomes. Keywords- Niosomes, Compositions, Preparation methods, Factors affecting, characterizations, in- vitro methods, Applications

Formulation and Evaluation of Clindamycin phosphate Niosomes by using Reverse Phase Evaporation Method

The formulate and evaluate Niosome drug delivery system for Clindamycin phosphate to increase its effectiveness by increasing penetration through skin and reducing its side effects Sorbitan esters which are Non-ionic surfactants was the key ingredient which forms vesicles upon hydration with aqueous media. Cholesterol was used to make vesicle stable and rigid. Different formulations were preparing by using different sorbitan ester and changing the ratio of surfactant and Cholesterol. Clindamycin Phosphate is an antibiotic widely used for the treatment of acne. The pseudomonas colitis occurs with oral dosage form while in topical dosage forms it has side effects like irritation, skin rash, itching etc. its topical bioavailability is also less. An attempt has been made to overcome these limitations for the preparation to prepare niosomes of clindamycin phosphate as well as for the enhanced delivery through skin by the variation in cholesterol level. Niosome were prepared by reverse phase evaporation method using span 60 as polymer. The compatibility of drug and polymer is analyzed by using FTIR and DSC method. There was no interaction detected by FTIR, DSC study. Further the prepared niosomes were evaluated for drug entrapment efficiency, drug content, and in vitro drug release. Amongst all the formulation batch 3 shows the best release when compared to other batch. SEM (Scanning electron microscopy) revealed that niosomes were spherical and porous. Finally it was concluded that clindamycin phosphate have been found suitable for controlled release formulation due to its bioavailability and biodegradability and thus lead to improved patient compliance. Keywords: Niosomes, Clindamycin Phosphate, Reverse phase evaporation method, Span60

Novel Strategy: Microsponges for Topical Drug Delivery

Microsponge delivery system is a unique and effective technology for the controlled release of topical agents. It is highly cross- linked porous, polymeric microspheres that can entrap wide range of active agents and in response to trigger or stimuli and release them onto the skin over a time. It consists of micro-porous beads, typically 5-300µm in diameter that acquire the flexibility to entrap a wide variety of active ingredients such as fragrances, sunscreens, emollients, anti-fungal, anti-infective, and anti-inflammatory agents etc., that are mostly used to prolong the topical administration of the drug . Recently it was investigated that microsponges also used for oral drug delivery system. The topical agent formulation with microsponge delivery system can be prepared in many different forms, such as cream, gel, or lotion. When the formulation is applied to the skin, the MDS releases its active ingredients on a time and in response to other stimuli (rubbing, temperature, pH etc.). They reduce side effects, enhance stability and modify drug release. Because of the size of the microsponges they cannot pass through the stratum corneum, so they remain on the skin surface and slowly releasing the active ingredients over a period. Slow rate of release from MDS reduce the irritancy associated with the topical agents. Slow and gradual release pattern of MDS prevents excessive build-up of the active agents in the epidermis and dermis. Therefore, these particles, remains on the surface of the skin and its fine lines delivering the active over prolonged time.                                                                      Keywords: Microsponge Delivery System, Quasi- emulsion solvent diffusion

Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators

Abstract Glucokinase (GK) is the key enzyme expressed in β-cells of pancreas and liver hepatocytes and helps in the maintenance of blood glucose levels in normal range. Activators of GK are the novel category of drug candidates which activate GK enzyme allosterically and show their antidiabetic activity. A new series of 3,5-disubstituted benzamide analogues was designed, synthesized and evaluated as GK activators by in vitro assay as well as in silico docking studies followed by evaluation of antihyperglycemic activity in animal model. Amongst the synthesized derivatives, compounds 5c, 5f, 5i, 6c, 6e and 6h displayed excellent in vitro GK activation. Compounds 6c and 6e exhibited highest antihyperglycemic activity in oral glucose tolerance test in animal model. Compound 6e displayed most significant antihyperglycemic activity and comparable to that of standard drug in animal studies. In addition, antihyperglycemic activity of the synthesized molecules was further supported by the in silico docking studies of the synthesized derivatives in the allosteric site of GK protein

THE Formulation and Characterization of Transdermal Patch of Candesartan Celexitil

The aim of the present study is to formulate and characterized the transdermal patch of Candesartan celexitil. The objective is study was to increase the bioavailability of drug. In the present study, transdermal patch of Candesartan celexitil were prepared  by solvent casting technique employing HPMC cps 50 polymer and glycerin as plasticizer using mercury as substrate. Total thirteen formulation (F1-F13) were prepared having drug and polymer ratio (1:2, 1:4, 1:6, 1:8, and 1:10). From the selected batch F2 containing drug polymer ratio (1:4), four formulations each were prepared and evaluated containg drug urea (1-4%) and oleic acid (1-4%) as permeation enhancer. The prepared transdermal patches were evaluated on the basis of different parameters like weigh, thickness, folding endurance, percent moisture absorption, percent moisture loss, drug content uniformity, in vitro skin permeation study. The fabricated final transdermal patches were further subjected to in vitro permeation study. In order to confirm the exact mechanism of drug release from all the patches, the data were computed and graphed according to Korsmeyer equation. Diffusion exponent of release process controlled by Super case Ⅱ transport Non- Fickian diffusion, n values of Korsmeyer- Peppas model shows a combination of diffusion and dissolution mechanism indicating the drug release from the formulation was controlled by more than one process. It was concluded that the prepared formulation F13 (4% w/v of oleic acid) showed highest cumulative percent drug release and increase the bioavailability of the drug. Keywords: Novel drug delivery system, Transdermal drug delivery, Transdermal drug delivery system, Differential scanning calorimetry