Release Dosage Form Research Articles

A Recent Update on Formulation and Development of Gastro-Retentive Drug Delivery Systems

Oral route has been the most convenient and accepted route of drug delivery. Owing to tremendous curative benefits of the oral controlled release dosage forms are being preferred as the interesting topic in pharmaceutical field to achieved improved therapeutics advantages. Gastro retentive drug delivery system is novel drug delivery systems which has an upper hand owing to its ability of prolonged retaining ability in the stomach and thereby increase gastric residence time of drugs and also improves bioavailability of drugs. Concept of novel drug delivery system arose to overcome the certain aspect related to physicochemical properties of drug molecule and the related formulations. In this context, various gastro retentive drug delivery systems have been used to improve the therapeutic efficacy of drugs that have a narrow absorption window, are unstable at alkaline pH, are soluble in acidic conditions, and are active locally in the stomach. Concept of novel drug delivery system arose to overcome the certain aspect related to physicochemical properties of drug molecule and the related formulations. Various approaches are currently used including gastro retentive floating drug delivery systems, swelling and expanding system, polymeric bio adhesive systems, modified shape systems, high density system and other delayed gastric emptying devices. Moreover, future perspectives on this technology are discussed to minimize the gastric emptying rate in both the fasted and fed states. The present review briefly addresses the physiology of the gastric emptying process with respect to floating drug delivery systems. The purpose of this review is to bring together the recent literature with respect to the method of preparation, and various parameters affecting the performance and characterization of floating microspheres. Attempt has been made to summarize important factors controlling gastro retentive drug delivery systems. Overall, this review may inform and guide formulation scientists in designing the gastro retentive drug delivery system.

Antifungal Drugs Loaded Nanosponges to Improve Bioavailability of Antifungal Drugs; A Review

Fungal infections have become a major concern in this era for human health leading to morbidity and mortality. A lot of antifungal agents are available for treatment, with poor therapeutic outcomes due to poor bioavailability, toxicity, and resistance challenges. Ordinary dosage forms are unable to meet the clinical needs. Nanosponges provide a promising drug delivery system overcoming major challenges concerned with antifungal agents. Nanosponges improves solubility, permeation, taste masking and stability of antifungal agents. It serves as an important tool for providing controlled release dosage forms. The nanosponges are easier to formulate and convenient for bilk manufacturing. Nanosponges thus provide various benefits to clinician to cope the overcoming demand of fungal infectious disease.

Assessment of physicochemical properties and comparison of the dissolution profile of amoxicillin caplets

Background: Marketed drugs must meet the required standards to guarantee product quality. Amoxicillin is a generic compound marketed under various trademarks as copy drugs. Amoxicillin caplets are an immediate release dosage form of BCS class I. An essential aspect of evaluating copy drugs is to assess the equivalence for their treatment to the innovator drugs to ensure the safety and effectiveness of the circulating copy drugs. Objective: The study aims to evaluate the physicochemical properties and compare the dissolution profile of amoxicillin caplets available in the market. Methods: Five amoxicillin caplet products, four test products, and one reference product were tested for their physicochemical properties and dissolution. The dissolution test was carried out with a type II device at a speed of 75 rpm in 900 mL of media buffered at pH 1.2, 4.5, and 6.8 and at a temperature of 37 +/- 0.5degrees celcius. The dissolution profile was analyzed by comparing it with the similarity factor (f2) parameters. Results: Two of the four amoxicillin caplet products had a similar dissolution profile to the reference products, namely products A and B. Products C and D were dissimilar because f2 was lower than 50 at pH 4.5. The caplets tested had almost the same dimensions, and all caplets met the requirements for uniformity of content, hardness, disintegration time, and dissolution. Conclusion: Not all of the amoxicillin caplets in the market have a similar dissolution profile to the reference products. Keywords: caplets, amoxicillin, dissolution, similarity factor

Isolation and Characterization of Dillenia Fruit Mucilage: A Novel Polymer for Microspheric Delivery of Losartan Potassium

Objective: The present investigation was aimed to isolate, characterize and establish a natural polymer obtained from partially ripe and fresh fruits of Dillenia indica and its utility to deliver losartan potassium in a sustained manner from microspheric macromolecular dosage form. Methods: All the microspheres were prepared by ionotropic gelation technique and investigated for various physico-chemical parameters along with in-vitro drug release studies to optimize the concentration of algino-Dillenia polymeric blend required to develop twice daily sustained release dosage form of losartan potassium. Results: The functional characteristic studies and rheological behavior analysis suggested that extracted polysaccharide can be used as a viscosity modifying agent as well as sustain release ingredient. All the microsphere formulations exhibited excellent mucoadhesion properties and site-specific drug release. In-vitro studies revealed that the optimum concentration of algino-Dillenia polymeric blend is suitable to deliver losartan potassium in a sustained manner for a prolonged period of time. SEM study revealed that the microspheres were spherical in shape with a smooth outer surface having small cracks. XRD and DSC studies revealed that losartan potassium is present as an amorphous form in the prepared optimized microsphere formulation. Conclusion: Thus, the present studies demonstrated that Dillenia fruit mucilage has an interesting rheological behavior which may be used as a viscosity modifying agent and exhibit promising properties of a sustained release dosage form to deliver losartan potassium from its microspheric dosage form.

Stable solid dispersion of lurasidone hydrochloride with augmented physicochemical properties for the treatment of schizophrenia and bipolar disorder.

Crystalline solid dispersion of lurasidone hydrochloride (LH) was made with various polar and non-polar small molecules to overcome the poor aqueous solubility issue. LH-Glutathione (GSH) solid dispersion in 1:1 ratio was prepared by co-grinding method and characterized by using differential scanning calorimetry (DSC), powder X-ray diffraction, Fourier transform infrared spectroscopy (FTIR) and Raman spectroscopy. GSH acts as antioxidant and reported for anti-schizophrenic activity may provide synergistic action with LH or reduce the side effects. LH in LH-GSH solid dispersion (SD) has shown improvement in solubility by 7.9 folds than plain drug which translated in terms of improved dissolution rate by two-folds. The in vitro dissolution results showed maximum dissolution rate with LH-GSH SD (97.85 ± 2.40%) compared to plain drug (50.5 ± 3.02%) at 15 min (t15 min, %) and thus, satisfying criteria of immediate release dosage form. DSC and FTIR data confirmed the stability of LH-GSH SD for 3 months at accelerated stability condition (40 ± 2°C and 75 ± 5% RH). The prepared LH-GSH SD can be used as a tool to target dual problems that is, enhanced physicochemical properties along with possible management of disorder which could be due to synergism with co-administered GSH. This approach is thought to be efficiently providing the relief to the psychological patients.

Gliclazide: Biopharmaceutics Characteristics to Discuss the Biowaiver of Immediate and Extended Release Tablets

The lists of essential medicines of the World Health Organization (WHO) and Brazil include gliclazide as an alternative to the oral antidiabetic drug of first choice, metformin, in the treatment of type 2 diabetes mellitus because of its pharmacokinetic profile and few side effects. Thus, it is also considered by WHO and the International Pharmaceutical Federation (FIP) as a drug candidate to biowaiver, which is the evaluation of how favorable the biopharmaceutics characteristics are in order to obtain waiver from the relative bioavailability/bioequivalence (RB/BE) studies to register new medicines. This paper presents a review about the solubility, permeability and dissolution of gliclazide. A critical analysis of the information allowed to identify gliclazide as a Biopharmaceutics Classification System (BCS) Class II drug. Therefore, new drugs in immediate release dosage forms will not be eligible for biowaiver. Regarding the extended release dosage forms, besides the limited solubility, no information on the comparative dissolution profile was found, which would be necessary to analyze a possible biowaiver for a smaller dosage. It can be concluded that the registration of new medicines containing gliclazide must undergo RB/BE studies, since there is not enough evidence to recommend the replacement and waiver of such studies for immediate and extended release formulations.

Thermal Sintering: A Novel technique in Formulation of Controlled Release Dosage form

Thermal Sintering: A Novel technique in Formulation of Controlled Release Dosage form

Development of immediate release (IR) 3D-printed oral dosage forms with focus on industrial relevance

Pharmaceutical 3D-printing represents a potentially new dosing and manufacturing approach for the pharmaceutical industry, with unique opportunities for personalization of dosage strengths. Fused deposition modelling (FDM) is a 3D-printing technique, which presents advantages for decentralized on-site manufacturing in hospitals and pharmacies. This study introduces industrially relevant development of formulations for filaments with the required mechanical properties to be 3D-printable and providing immediate release (IR) dosage forms using safe materials approved also for pediatric use. Hydroxypropyl-cellulose (HPC) SSL was chosen as hydrophilic polymer and caffeine with a load of 5-20% as thermally stable model drug. Poly-(vinyl pyrrolidone-vinyl acetate) copolymer (Kollidon VA64) and poly-(vinyl alcohol-polyethylene glycol) graft copolymer (Kollicoat IR) were additional water-soluble polymers tested in combination with HPC and xylitol and polyethylene glycol (PEG) 4000 were evaluated as hydrophilic plasticizers and PEG4000 and maltodextrin as pore formers. Formulations were hot-melt extruded using a scalable twin-screw extruder and 3D-printed into honeycomb geometry solid dosage forms with high (100%) and low (80%) infill density. Rapid or very rapid release was achieved via formulation selection and tablet design parameters. PEG4000 in combination with Kollidon VA64 demonstrated superior processability and significantly accelerated release properties of the matrix independently of infill density. Lowering caffeine content improved hot-melt extrusion processability for each formulation but prolonged dissolution. The use of Kollicoat IR resulted in superior mechanical properties of the manufactured filaments, with easy handling and successful 3D-printing for drug load of 5 to 20%. For most formulations, lowering infill density of 3D-printed tablets yielded faster drug dissolution in agreement with the literature. However, the extent of the infill density effect varied depending on formulation. Caffeine was present in stable crystalline state in 3D-printed tablets. Printing temperature appeared to be critical for drug dissolution in vitro. This wide-ranging excipient investigation epitomizes the beginning of a toolbox approach targeting FDM processability in combination with immediate release characteristics of personalized dosage forms.

Sustained release dosage form of noscapine HCl using hot melt extrusion (HME) technique: formulation and pharmacokinetics.

Sustained release formulation of noscapine (Nos) HCl could be useful in maintaining plasma Nos HCl level for prolonged period of time, which is important for chemo-sensitization. However, weakly basic drugs like Nos HCl have pH-dependent solubility. Therefore, the purpose of this study was to achieve pH-independent drug release by developing the sustained release dosage form of Nos HCl using biodegradable polymer Eudragit RLPO and FDA-approved pH modifier citric acid (CA) by hot melt extrusion (HME) technique. Nos HCl was successfully formulated using 10% CA with 91.2 ± 1.34% drug recovery through the extruder. X-ray diffraction (XRD) results showed that drug was completely dispersed in the polymer and changed to amorphous from its crystalline form. In vitro drug release studies in pH 6.8 buffershowed that formulation containing 10% CA released 70.99 ± 3.85% drug in 24h after initial burst release of 40.04 ± 2.39% compared toformulation without CA. Furthermore, in vivo pharmacokinetic data showed the sustained release plasma concentration time curve with significant (p < 0.05) increase in area under curve (AUC) in NosHCl extrudate compared toNos HCl solution. Overall, HME can be used to enhance the bioavailability and achieve the pH-independent solubility of weakly basic drugs like Nos HCl. Graphical abstract.

Impact of Tablet Shape on Drug Dissolution Rate Through Immediate Released Tablets.

Purpose: The aim of this study was to evaluate the influence of the geometric shape on the dissolution rate of the domperidone, a drug model for immediate release dosage form. In this regard, a lack of sufficient information about the effective dissolution rate of the drugs regarding their shapes has made this issue an interesting subject for researchers. Methods: For this purpose, three tablet shapes, namely flat and biconvex both in a round and oblong shapes, with different four sizes were modelled for the preparation of domperidone tablet. In vitro dissolution test was accomplished using a USP dissolution apparatus II. The drug dissolution rate was assessed by calculating various dissolution parameters; e.g., dissolution efficiency (DE), mean dissolution rate (MDR), mean dissolution time (MDT), and difference and similarity factors (f1 and f2 ). Results: Regarding the disintegration time, the larger tablets showed a faster disintegration time. When the size of the tablets was smaller, the amount of released drug was significantly decreased. In addition, #9 tablets with a flat or biconvex geometry had obvious effects on the DE values. Generally, biconvex tablets had higher DE percentage than the flat tablets. Conclusion: Noticeable differences in dissolution parameters by considering the different geometric shapes play an important role in the drug release kinetics which makes a significant effect on quick onset of action in oral administration.

Formulation of Sustained Release Hydrophilic Matrix Tablets of Tolcapone with the Application of Sedem Diagram: Influence of Tolcapone's Particle Size on Sustained Release.

Hydrophilic matrix tablets are a type of sustained release dosage form characterized by distributing a drug in a matrix that is usually polymeric. Tolcapone is a drug that inhibits the enzyme catechol-O-methyl transferase. In recent years, it has been shown that tolcapone is a potent inhibitor of the amyloid aggregation process of the transthyretin protein, and acts by stabilizing the structure of the protein, reducing the progression of familial amyloid polyneuropathy. The main objective of this study was to obtain a sustained release tablet of tolcapone for oral administration with a preferred dosage regimen of 1 administration every 12 or 24 h and manufactured, preferably, by direct compression. The SeDeM Diagram method has been used for the formulation development of hydrophilic matrix tablets. Given the characteristics of tolcapone, the excipient selected for the formation of the polymeric matrix was a high viscosity hydroxypropylmethylcellulose (Methocel® K100M CR). A decrease in the particle size of tolcapone resulted in a slower dissolution release of the formulation when the concentration of the polymer Methocel® K100M CR was below 29%. These surprising and novel results have given rise to patent number WO/2018/019997.

Assessing the potential bioequivalence requirement for oral immediate release dosage form: Post approval changes for cardiovascular drugs

Formulation changes can occur during drug development before approval or after approval. Recently, the FDA issued several guidances regarding scale up and post approval changes (SUPAC). The first of the series addresses the requirements for determining and evaluating those changes for immediate release (IR) oral dosage form. In that guidance, the concepts of Biopharmaceutical Classification System (BCS) were introduced. Based on their solubility (S) and permeability (P), the drugs are classified as high (H) and low (L), and thus are divided into four classes (HS/HP, HS/LP, LS/HP, and LS/LP). Only LS/LP drugs are required to perform a bioequivalence (BE) study. The other classes of drugs are required to perform a BE study only when they fail their dissolution testing, under level 3 changes in manufacturing process, components and composition. In addition, only a handful of drugs were classified under the BCS system. In order for the industry to extensively apply the BCS system, more drugs need to be classified. The objective of this study is to compile the pertinent information relating to the drug release from the formulation and absorption through the gut wall. By evaluating the information collectively, an educational guess can be made as to whether the formulation can be rapidly converted to solution in the gastrointestinal tract and therefore behave as such. Under those conditions, a BE study may not be needed if in vitro dissolution performance can be demonstrated. Cardiovascular drugs were studied for their vastly different safety profiles, physicochemical properties and pharmacokinetic behaviors. This report is written for the Taiwan regulatory authority (Bureau of Pharmaceutical Affairs, Department of Health) considering the uniqueness of the Asian pharmaceutical environment. The final judgement was made based on the following information: 1) effective and toxic concentrations; 2) solubility and pKa; 3) total % absorption as both drug and metabolite(s); 4) half-life and its peak time as indication of in vivo solubility and permeability of drug; and 5) German BA list, WHO list, and the FDA narrow therapeutic index drug list. The reason(s) for the judgement was provided.

The effect of Eudragit and enteric polymer composite on the release of nicardipine

The purpose of this study was to investigate the sustained release of nicardipine/polymer solid dispersions prepared by solvent evaporation method. The release pattern of drug from solid dispersions was evaluated by the dissolution test in both dissolution medium of phosphate buffer pH 6.8 or gastric acid fluid pH 1.2, and was compared with a commercial long acting product Perdipine®. The results showed that the formulations with lower ratio of Nicardipine/Eudragit RS (N/RS) (below 1/ 5) had sustained release effect in gastric acid fluid (pH 1.2). The release rate of formulation of N/RS = 1/5 was slightly faster than that of Perdipine® in gastric acid fluid in the early stage. On the contrary, the release rate was lower than that of Perdipine® in phosphate buffer (pH 6.8). The enteric polymers such as HPMCAS-LF grade (HPMCAS) and hydroxypropyl methylcellulose phthalate, HP-55 grade (HPMCP) were incorporated into the formulation of NC/ERS = 1/5 solid dispersion to improve the drug release in both dissolution medium. It was found that the dissolution efficiencies of drug were increased 2.35-21.08 folds with the addition of 20-40% of enteric polymer in pH 6.8 media. Among these formulations of N/RS/HPMCP = 1/3.5/1.5 had similar dissolution pattern with Perdipine® in either medium of phosphate buffer or gastric acid fluid (f2 values were above 50), showing that the sustained release dosage form of nicardipine solid dispersions could be developed by using the combination of Eudragit RS and enteric polymer.

Oral Modified Drug Release Solid Dosage Form with Special Reference to Design; An Overview.

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 and this oral route provides maximum active surface area among all drug delivery system for administration of various drugs. The attractiveness of these dosage forms is due to awareness of toxicity and ineffectiveness of drugs when administered by oral conventional method in the form of tablets and capsules. Usually, conventional dosage form produces wide range of fluctuation in drug concentration in the bloodstream and tissues with consequent undesirable toxicity and poor efficiency. The maintenance of concentration of drug in plasma within therapeutic index is very critical for effective treatment. These factors as well as factors such as repetitive dosing and unpredictable absorption lead to the concept of oral modified drug delivery systems like Sustained release, prolonged release, modified release, extended release. These formulations are used to identify drug delivery systems that are designed to achieve or extend therapeutic effect by continuously releasing medication over an extended period of time after administration of a single dose. This review describes the basic information regarding modified release dosage form like designed to release their medication in controlled manner, criteria for selecting modified release dosage form and factors influencing the dosage and release pattern.

Formulation and Evaluation of Fast-disintegrating Tablets of Flurbiprofen and Metoclopramide

The present study was aimed to formulate and evaluate fast-disintegrating tablets (FDTs) having Flurbiprofen (FP) and Metoclopramide HCl (MHCl) in combination. Direct compression was used to formulate FDTs of FP and MHCl as a combination regimen in six formulations. FDTs are defined as solid oral dosage form that disintegrates rapidly within seconds when placed in the oral cavity. FDT-1, FDT-2, FDT-3, FDT-4, FDT-5, and FDT-6 were formulated using crospovidone, croscarmellose sodium, and sodium starch glycolate as superdisintegrants each in two formulations. Several pre-compression tests (angle of repose, bulk density, tapped density, Hausner’s ratio, and compressibility index), post-compression evaluation (weight variation, friability, hardness, disintegration time, wetting time, assay, in vitro dissolution study, release kinetics study, statistical analysis, and stability study), and drug compatibility study were done for all six formulations. Pre-compression evaluation showed good flow properties of powder blend. Drug compatibility study showed no interactions between active drugs and excipients. Disintegration and wetting time of all the formulations were in seconds indicating immediate release of drug. Optimized formulation (FDT-6) containing sodium starch glycolate in 15 mg gave 100% release in 15 min for MHCl and in 20 min for FP. Optimized formulation was found stable after being placed at accelerated stability conditions for 6 months. Release kinetics study showed that all formulations followed Korsmeyer-Peppas model indicating drug release from modified release dosage form. Statistical analysis revealed no significant difference statistically (p > 0.05) between drug release rate of all prepared formulations. FDTs improved the release rate that assured that this tactic may be beneficial to increase the dissolution rate of FP and MHCl in order to increase patient compliance.

Effect of Common Excipients on Intestinal Drug Absorption in Wistar Rats.

The aim of the present paper is to study the effect of common excipients on the permeability of atenolol (as drug absorbed mainly by passive diffusion) and rhodamine (as P-glycoprotein substrate). The apparent permeability was measured by an in situ perfusion method in Wistar rats using the closed loop Doluisio's method. Permeability values were characterized in the absence and presence of 18 commonly used excipients. Excipient concentrations were selected based on the amounts in oral immediate release dosage forms, which failed the test during the human bioequivalence studies. Atenolol was studied with and without excipients in the whole small intestine, whereas rhodamine was tested in three different intestinal segments to account for the differential expression of P-glycoprotein, and it was further on tested in the ileum, in the presence of excipients. Atenolol presented higher permeability values when it was administered with colloidal silica, croscarmellose, hydroxypropyl methylcellulose (HPMC), magnesium stearate, MgCO3, poly(ethylene glycol) 400, poly(vinylpyrrolidone), sorbitol, starch, and TiO2 rhodamine showed higher permeability values when it was administered with croscarmellose and HPMC. On the one hand, the mechanisms of action were not discernible with the proposed experiments. On the other hand, commercial formulations do not present a single excipient but several, which can counteract their effects. The in situ perfusion technique can be useful for a preliminary screening and risk analysis, while the in vivo pharmacokinetic results would be needed to define conclusive effects.

Development and Optimization of Naproxen Sodium Controlled Release Tablets: QbD Approach

Abstract: Objectives: The aim of present study was to formulate and optimize Multi-unit Naproxen Sodium controlled release tablet by QbD approach. Controlled release dosage form for naproxen sodium was selected to reduce dosing frequency and gastrointestinal side effects of drug. Methods: Naproxen Sodium CR tablets were prepared by using wet granulation method by employing Quality by Design (QbD). This tablet was made by a mixture of a granulate having an immediate release with a granulate having a controlled release, in terms of the active ingredient. Eudragit RSPO and RLPO polymers were used to control the drug release. Optimization of tablet formulation was done using 23 factorial design to study the effect of concentration of Eudragit RSPO, Eudragit RLPO polymers and concentration of disintegrating agent i.e. crospovidone on disintegration time and f2 factor of drug released. Tablets were evaluated for thickness, hardness, friability, assay and drug release. Results: Optimized formulation shows controlled drug release profile upto 14 hrs. with disintegration time of 88 min. Conclusion: It was concluded that tablet formulation of Naproxen Sodium CR tablets employing QbD leads to a single dose per day in the management of rheumatoid arthritis and also concluded that Eudragit RLPO and Eudragit RSPO polymers can be successfully used to controlled drug release profile of tablet. Key words: Multi-unit-controlled release system, Quality by Design, Design of experiment, Eudragit RLPO, Eudragit RSPO.

Folic acid modified gold nanoparticle for targeted delivery of Sorafenib tosylate towards the treatment of diabetic retinopathy

Preparing a controlled release dosage form for specific locations within the body is one of the most challenging tasks in the present times. Moreover, green synthesis of metal nanoparticles is attaining greater significance because of their high biocompatibility and negligible toxicity. Gold nanoparticles, among them, are considered to be one of the best modes of drug delivery system for the treatment of various diseases. The excellent properties of gold nanoparticles make them a potential carrier for carrying and releasing drugs at the specified location in a controlled manner. In this research, gold nanoparticle (AuNPs) has been prepared by green synthesis for the treatment of diabetic retinopathy. These AuNPs has been further modified with FA-b-PEG copolymer for the targeted delivery of the drug Sorafenib tosylate. The selected drug works on VEGF receptors in the region of retinal neovascularisation. The optimized dosage form prepared from gold chloride and ginger extract has been characterized. Histopathological studies as well as fundus photography has been used for the in-vivo characterisation of the prepared dosage form and it has been found that it can be quite an effective treatment for retinal neovascularisation in patients of diabetic retinopathy.

Topical delivery of Tacrolimus using liposome containing gel: An emerging and synergistic approach in management of psoriasis

Psoriasis is a chronic relapsing inflammatory and hyperproliferative skin disease affecting quality of life. It affects an estimated 8 million Americans and more than 125 million people worldwide. The estimated cost to treat psoriasis in USA is over 13 billion US dollars per year. Treatment of psoriasis may include topical steroid-sparing agent, topical corticosteroids, phototherapy or biologics. Tacrolimus has 10-fold greater immunosuppressive activity than the ciclosporin A which has been recommended for effective treatment of psoriasis. However, it has been widely investigated using conventional formulation approaches which limit its clinical outcomes. It has poor cutaneous bioavailability when administered topically using conventional delivery approach, thus it has poor efficacy against the psoriasis. Low aqueous solubility and high degradation of Tacrolimus make it difficult to formulate as a liquid preparation. Moreover, Tacrolimus has narrow therapeutic index and thus it is essential to prevent its possible toxic effects when a modified release dosage form is administered. The present hypothesis aims to put forward to incorporate Tacrolimus into a novel lipid based nanocarrier system, which would be further loaded into a hydrogel base and evaluated for its target specific topic delivery. Due to the structural similarity of the lipid nanocarriers and skin, these vesicles would target the skin tissues effectively and treat psoriasis with minimum or no side effects. Thus, the proposed formulation would be a considerable value addition to the current therapeutic approaches used for psoriasis management.

Controlled Release Gel Encompassing Curcumin Microspheres and Diclofenac Diethylamine for Feat Against Arthritis Inflammation.

Diclofenac and curcumin is anticipated to have synergistic action. Hence, topical route of administration can be used in minimizing the issues with oral administration of both drugs. This research aims at formulation of controlled release dosage form containing curcumin microspheres and diclofenac diethylamine and then incorporating it into gel formulation for treatment of inflammation associated with rheumatoid arthritis. Curcumin microspheres were prepared, optimized and assayed. Gel containing microspheres was formulated and evaluated for physicochemical parameters like spreadability and viscosity. In vitro and ex vivo diffusion studies were carried out followed by evaluation of efficacy. Efficacy of the developed formulation was evaluated for anti-inflammatory activity. Particle size, Zeta potential, pH, spreadability and viscosity of optimized Batch F1 was found to be in range 0.5 µm - 5 µm,-27.9 mV, 6.2, 105 g cm/s and 7500 cps respectively. In vitro diffusion of developed gel of diclofenac diethylamine and curcumin was found to be 92.16 ± 0.0040 % in 3 h and 92.54 ± 0.0036 % in 12 h as compared to 79.57 ± 0.004 % diffusion in 2 h for marketed gel, thus showing controlled delivery of curcumin. Decreased inflammation in formulation treated group by 72.53% and 50.75% in marketed treated group was seen. Thus the formulation developed showed prolonged activity as well as better anti-inflammatory activity.