Eudragit RL Research Articles

D-optimal mixture design inspired modified release tablet formulation of lamotrigine for the treatment of seizures: An in-depth characterization

Lamotrigine (LTG) an anticonvulsant drug with a dissociation constant (pKa: 5.7), suffers from enhanced blood plasma spike after each dose, when administered as fast release tablet. Being BCS class-II candidate and pH dependent solubility, development of release-controlled tablets of LTG is a major challenge. This investigation aims at designing the release-controlled tablet (RCT) formulation of LTG using a solid dispersion (SD) technique via addressing its solubility and release problems. RCT of LTG was fabricated using SD blend of Eudragit RL and Eudragit RS and PVP K-30 with different polymer blend ratio (1:5 and 1:7). The optimization of RCT of LTG was performed using D-optimal mixture design with three independent variables, three response variables, and one constraint. The dissolution rate was determined and data were then fitted to different mathematical models. Scanning electron microscopy (SEM) and X-ray diffraction (XRD) studies and tableting parameters were analyzed. In vitro studies of predicted optimized batches (POBs) have shown that drug release over a period of 12hours was 88.05±3.4% in media I, 86.10±3.7% in media II and 85.84±4.2% in media III. An in vitro kinetic model equating R2-value for all the tested models indicated that the first order and Higuchi release kinetics model were the most appropriate. Based on the optimized formulation consisting of SD of LTG with Eudragit RL, Eudragit RS and PVP K-30, the release rate was consistently similar throughout the GI tract, regardless of the pH of the environment.

The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets.

Cobalamin (vitamin B12), an essential vitamin with low oral bioavailability, plays a vital role in cellular functions. This research aimed to enhance the absorption of vitamin B12 using sublingual mucoadhesive tablets by increasing the residence time of the drug at the administration site. This research involved the preparation of different 50 mg placebo formulas using different methods. Formulas with disintegration times less than one minute and appropriate physical characteristics were incorporated into 1 mg of cyanocobalamin (S1-S20) using the direct compression method. The tablets obtained were evaluated ex vivo for residence time, and only those remaining for >15 min were included. The final formulas (S5, S8, S11, and S20) were evaluated in several ways, including pre- and post-compression, drug content, mucoadhesive strength, dissolution, and Permeapad® permeation test employed in the Franz diffusion cell. After conducting the evaluation, formula S11 (Eudragit L100-55) emerged as the most favorable formulation. It exhibited a mucoadhesive residence time of 118.2 ± 2.89 min, required a detachment force of 26 ± 1 g, maintained a drug content of 99.124 ± 0.001699%, and achieved a 76.85% drug release over 22 h, fitting well with the Peppas-Sahlin kinetic model (R2: 0.9949). This suggests that the drug release process encompasses the Fickian and non-Fickian kinetic mechanisms. Furthermore, Eudragit L100-55 demonstrated the highest permeability, boasting a flux value of 6.387 ± 1.860 µg/h/cm2; over 6 h. These findings indicate that including this polymer in the formulation leads to an improved residence time, which positively impacts bioavailability.

IMPLICATION OF CENTRAL COMPOSITE DESIGN IN THE DEVELOPMENT OF SIMVASTATIN-LOADED NANOSPONGES

Objective: The present study’s objective was to apply a central composite design to develop the simvastatin-loaded nanosponge formulation to improve its oral bioavailability. Methods: With the help of a design expert (State-Ease version 13.0.1), a central composite design was selected for the formulation of simvastatin-loaded nanosponges by using a defined concentration of Eudragit L-100 (X1) and PVA (X2) as independent variables and particle size (Y1), percent (%) entrapment efficiency (EE) (Y2), in vitro drug release (Y3) as dependent variables. Fourteen (SF1-SF14) formulations were prepared using the emulsion solvent evaporation and evaluated for surface morphology, particle size, drug-excipient compatibility, %EE, and % drug release. The optimized model (SF14) obtained from a design expert was evaluated for in vivo pharmacokinetics in animal models. Results: SF14 was formulated and evaluated for morphology (shape and size) of the particle, % EE, in vitro % drug release, and its kinetics. The formulation showed particle size of 163±0.45 nm, 80.54 %±0.57 of EE, and 97.13%±0.38 of drug release at 8h. The release kinetics followed the zero-order and Higuchi mechanisms with non-fiction diffusion. In vivo results showed Cmax, Tmax, AUC0-t, AUC0-α, and MRT0-α for nanosponges were 0.175 µg/ml, 6 h, 1.561 µg/mlh, 1.755 µg/mlh, 11.77 h, respectively. Conclusion: The results indicated a significant increase in the bioavailability of the drug in nanosponges compared with standard drugs. The experimentally designed nanosponge formulations have been successfully developed, and evaluated parameters show that the nanosponge formulation of Simvastatin is a promising delivery through the oral route.

Suitability of Wurster-Fluid Bed technique for functional Eudragit L-100 coating on tablet cores

Suitability of Wurster-Fluid Bed technique for functional Eudragit L-100 coating on tablet cores

Design, development, and evaluation of spray dried flurbiprofen loaded sustained release polymeric nanoparticles using QBD approach to manage inflammation

Spray-dried Flurbiprofen (FLB) loaded polymeric nanoformulation using Eudragit L 100 and Ethylcellulose. They were optimized and evaluated. This study determined drug release (%) and encapsulation efficiency (%) by developing a nanoparticulate system using the design of experiment (DoE) approach. FLB is slightly soluble in water; it dissolves slowly and has a low oral bioavailability. FLB-loaded polymeric nanoparticles were produced by solvent evaporation and Spray drying technology. In this research, nanoparticle formulation was prepared by screening and optimization by approaching two different statistical methods (Plackett-Burman and Central composite Designs). The polymeric nanoparticles were evaluated for various characteristics, including drug release, percentage of encapsulation efficiency, X-ray diffraction (X-RD), surface morphology, and Fourier transform infrared (FTIR) spectroscopy. Based on the X-RD analysis, it was found that the drug was successfully incorporated into the polymeric nanoparticles. As a result of nanoparticles containing FLB, % Drug release values were found to be nearly 85-90% increased while % EE was observed in the range of 79-89%. An excellent sustained release, i.e., 14 h, is possible by combining Ethylcellulose (EC) and Eudragit L 100 (ED-100) polymers. The results are beneficial in identifying the ideal formulation parameters for effective encapsulation. Abbreviations: FLB: Flurbiprofen; API: Active pharmaceutical ingredient; DR: Drug release; EE: Encapsulation efficiency; DoE: Design of experiment; X-RD: X-ray diffraction; FTIR: Fourier transform infrared spectroscopy.; PVA: Polyvinyl alcohol; EC: Ethylcellulose; EUGD: Eudragit L 100; NPs: Nanoparticles; PBD: Placket- Burman Design; CCD: Central Composite Design; CMV: Critical method variables; GIT: Gastrointestinal track; SLN: Solid lipid nanoparticles; NLC: Nanostructured lipid carriers; NSAID: Nonsteroidal anti-inflammatory drug; BCS: Biopharmaceutical classification system; PS: Particle size; PDI: Polydispersity Index; ZP: Zeta potential; FE-SEM: Field emission scanning electron microscopy; 2D: 2 Dimensional; 3D: 3 Dimensional

Formulation and Evaluation of Mucoadhesive Beads of Dexamethasone

The goal of the current study was to formulate and evaluate mucoadhesive Dexamethasone beads to significantly lengthen the duration of the drug's stay in the GI system to treat Crohn’s disease. Dexamethasone is a corticosteroid that acts as an anti-rheumatic and anti-inflammatory. To decrease the dosage frequency Dexamethasone adhesive beads were formulated for Intimate contact with the underlying absorption surface is made possible by a prolonged stay at the location, which enhances the drug's therapeutic effectiveness. In the current study, calcium chloride and aluminium chloride were utilised as cross-linking agents to create Dexamethasone mucoadhesive beads employing adhesive polymers like sodium alginate, HPMC, and Eudragit L-100. The prepared beads' entrapment efficiencies ranged from 57.15 to 99.16%. Regarding entrapment effectiveness, particle size, surface properties, and in-vitro drug release experiments, the impact of bioadhesive polymers and cross-linking ions was assessed. The MPS-7 delayed the drug's release for 12 hours, which may be related to the cross-linking agent aluminium chloride. According to drug release kinetics, all of the formulations were more linear concerning zero order (r2=0.99) than concerning first order (r2=0.751 to 0.828). Super Case 2 Transport was discovered to be the precise release mechanism.

In Situ Cocrystallization via Spray Drying with Polymer as a Strategy to Prevent Cocrystal Dissociation.

The aim of the present study was to investigate how different polymers affect the dissociation of cocrystals prepared by co-spray-drying active pharmaceutical ingredient (API), coformer, and polymer. Diclofenac acid-l-proline cocrystal (DPCC) was selected in this study as a model cocrystal due to its previously reported poor physical stability in a high-humidity environment. Polymers investigated include polyvinylpyrrolidone (PVP), poly(1-vinylpyrrolidone-co-vinyl acetate) (PVPVA), hydroxypropyl methyl cellulose, hydroxypropylmethylcellulose acetate succinate, ethyl cellulose, and Eudragit L-100. Terahertz Raman spectroscopy (THz Raman) and powder X-ray diffraction (PXRD) were used to monitor the cocrystal dissociation rate in a high-humidity environment. A Raman probe was used in situ to monitor the extent of the dissociation of DPCC and DPCC in crystalline solid dispersions (CSDs) with polymer when exposed to pH 6.8 phosphate buffer and water. The solubility of DPCC and solid dispersions of DPCC in pH 6.8 phosphate buffer and water was also measured. The dissociation of DPCC was water-mediated, and more than 60% of DPCC dissociated in 18 h at 40 °C and 95% RH. Interestingly, the physical stability of the cocrystal was effectively improved by producing CSDs with polymers. The inclusion of just 1 wt % polymer in a CSD with DPCC protected the cocrystal from dissociation over 18 h under the same conditions. Furthermore, the CSD with PVPVA was still partially stable, and the CSD with PVP was stable (undissociated) after 7 days. The superior stability of DPCC in CSDs with PVP and PVPVA was also demonstrated when systems were exposed to water or pH 6.8 phosphate buffer and resulted in higher dynamic solubility of the CSDs compared to DPCC alone. The improvement in physical stability of the cocrystal in CSDs was thought to be due to an efficient mixing between polymer and cocrystal at the molecular level provided by spray drying and in situ gelling of polymer. It is hypothesized that polymer chains could undergo gelling in situ and form a physical barrier, preventing cocrystal interaction with water, which contributes to slowing down the water-mediated dissociation.

Development and Evaluation of Buccal Mucoadhesive patches of Losartan Potassium

Buccal mucoadhesive patches of losartan potassium were formulated using hydroxypropyl methyl cellulose grades - K4M, K15M, K50M and Eudragit L100 polymers by the method of solvent casting. The prepared formulations were characterized for mechanical and physicochemical parameters like thickness, surface pH, uniformity of weight, swelling index, folding endurance, percentage moisture loss, drug content, in vitro dispersion and in vitro residence time. Further, in vitro drug release study was performed with the use of freshly prepared egg membrane as the semi-permeable membrane. The best formulation (F6) exhibited higher percentage of drug release 97.26%±0.41 at the end of 8 h. The sustained release of losartan potassium was found to be attained up to 8 h duration.

Fabrication and Evaluation of Poly(2-hydroxyethyl methacrylate)/Eudragit L-100 Hydrogels with Fusidic Acid to Promote Eczema Treatment.

In this study, hydrogels containing 2-hydroxyethyl methacrylate (HEMA), Eudragit L-100, and fusidic acid in different compositions were prepared with the confinement method by using ammonium persulfate (APS) as a chemical initiator and ethylene glycol dimethacrylate (EGDMA) as a cross-linker to determine the most suitable formulation for use in eczema treatment. Fusidic acid (FA)-confined pHEMA/Eudragit L-100 in synthesis of the hydrogel was used with the Taguchi method, and the optimum synthesis conditions were determined. The swelling percentages of the hydrogels were calculated in different pH environments and distilled water. Also, the cream formulations developed and contained in chitosan and HEMA-based polymers were synthesized. Viscosity and pH values changed between 30,000 and 100,000 cP and between 5 and 6 for different cream formulations with various conditions, respectively. Also, swelling percentages of hydrogels were between 20 and 40. Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM) analyses were performed to characterize the hydrogel structure and the cream formulations. In addition, the stability of the formulations to 28 days and the changes in parameters such as appearance, centrifugation, pH, relative density, viscosity, spreading were evaluated, comparatively.

Study of anti-inflammatory and anti-arthritic potential of curcumin-loaded Eudragit L100 and hydroxy propyl methyl cellulose (HPMC) microparticles

Study of anti-inflammatory and anti-arthritic potential of curcumin-loaded Eudragit L100 and hydroxy propyl methyl cellulose (HPMC) microparticles

Factors That Influence Sustained Release from Hot-Melt Extrudates.

Hot-melt extrusion is a well-established tool in the pharmaceutical industry, mostly implemented to increase the solubility of poorly soluble drugs. A less frequent application of this technique is to obtain formulations with extended release. This study investigated the influence of polymer choice, drug loading, milling and hydrodynamics on the release of a model drug, flurbiprofen, from sustained-release hot-melt extrudates with Eudragit polymers. The choice of polymer and degree of particle size reduction of the extrudate by milling were the two key influences on the release profile: the percentage release after 12 h varied from 6% (2 mm threads) to 84% (particle size <125 µm) for Eudragit RL extrudates vs. 4.5 to 62% for the corresponding Eudragit RS extrudates. By contrast, the release profile was largely independent of drug loading and robust to hydrodynamics in the dissolution vessel. Thus, hot-melt extrusion offers the ability to tailor the release of the API to the therapeutic indication through a combination of particle size and polymer choice while providing robustness over a wide range of hydrodynamic conditions.

Formulation and optimization of theophylline-loaded enteric-coated spanlastic nanovesicles for colon delivery; Ameliorate acetic acid-induced ulcerative colitis

Treatment of colon diseases presents one of the most significant obstacles to drug delivery due to the inability to deliver sufficient drug concentration selectively to the colon. The goal of the proposed study was to develop, optimize, and assess an effective colon target delivery system of theophylline-based nanovesicles (TP-NVs) surrounded by a biodegradable polymeric shell of chitosan (CS) and Eudragit L100 (EL100) for the treatment of ulcerative colitis (UC). TP-loaded nanovesicles were fabricated using the ethanol injection method and coated with CS and EL100, respectively. We used a 32-factorial design approach to optimize the concentration of CS and EL100 to minimize particle size (PS) and maximize the cumulative amount of theophylline released (CTR) after 24 h. The optimized formulation was described using transmission electron microscopy (TEM), differential scanning calorimetry (DSC), and in vitro release. In-vivo quantification of theophylline in the gastrointestinal tract and in-vivo targeting potential in a rat model of acetic acid-induced colitis were also thoroughly evaluated. The characteristics of the optimal formula predicted by the 32-factorial design approach corresponded exceptionally well with the measured PS of 271.3 nm, the zeta potential of −39.9 mV, and CTR of 3.95, and a 99.93% after 5 and 24 h, respectively. Notably, the in vivo results in the rat model of colitis showed that the formulation with an optimized coat significantly improved theophylline distribution to the colon and markedly decreased the expression of interleukin-6 and ulcerative lesions compared to a pure theophylline solution. These outcomes elucidated the feasibility of a 32-factorial design to detect the crucial interactions between the study's components. Our findings suggested that enteric-coated nanovesicles formulations with optimal coat compositions of 0.2693% (w/v) and 0.75% (w/v) of CS and EL100, respectively, were promising carriers for colonic delivery of theophylline, a rate-limiting step in the treatment of UC.

Influence of the Polymer and Solvent Variables on the Nanoencapsulation of the Flavonoid Quercetin: Preliminary Study Based on Eudragit® Polymers

Eudragit® polymers have proven their potential as a means to control the release of aqueous insoluble drugs in various delivery systems as polymer nanoparticles (PNPs). The size (S) and polydispersity index (PDI) of PNPs are crucial factors for their interaction with biological systems from a pharmaceutical standpoint. This study aimed to determine the impact of the volumes of the organic phase (OP) and aqueous phase (AP), as well as the polymer amount (PA), on the size and PDI of PNPs prepared using the nanoprecipitation method for encapsulating quercetin (Qr). The study also evaluated the toxic effects of PNPs on human erythrocytes. The PNPs were prepared using preformed polymers derived from methacrylic acid and polyvinyl alcohol (PVA) as a surfactant. The nanoprecipitation technique enabled the production of particles smaller than 200 nm with a PDI lower than 0.2, and the study established the significant impact (p &lt; 0.05) of the three variables related to the polymers and solvents. The selected PNPs contained 5 mg of Qr and 50 mg of Eudragit polymers (1:10 w/w Eudragit® EPO, E100, L100, and Eudragit L100-55) and diverse concentrations of PVA. The study found that including PVA in the AP increased the Qr encapsulation by up to 98%. The hemolytic potential of Eudragit® PNPs and Qr was assessed in human erythrocytes, with no significant cytotoxic activity observed (p &lt; 0.001) compared with the control. In conclusion, via the nanoprecipitation technique, preparing PNPs with defined and homogeneous S to entrap the flavonol Qr efficiently is possible.

In-situ formation of nanoparticles from drug-loaded 3D polymeric matrices

The in-situ formation of nanoparticles from polymer-based solid medicines, although previously described, has been overlooked despite its potential to interfere with oral drug bioavailability. Such polymeric pharmaceuticals are becoming increasingly common on the market and can become even more popular due to the dizzying advance of 3D printing medicines. Hence, this work aimed to study this phenomenon during the dissolution of 3D printed tablets produced with three different polymers, hydroxypropylmethylcellulose acetate succinate (HPMCAS), polyvinyl alcohol (PVA), and Eudragit RL PO® (EUD RL) combined with plasticizers and the model drug naringenin (NAR). The components' interaction, dissolution behavior, and characteristics of the formed particles were investigated employing thermal, spectroscopic, mechanical, and chromatographic assays. All the systems generated stable spherical-shaped particles throughout 24 h, encapsulating over 25% of NAR. Results suggest encapsulation efficiencies variations may depend on interactions between polymer-drug, drug-plasticizer, and polymer-plasticizer, which formed stable nanoparticles even in the drug absence, as observed with the HPMCAS and EUD RL formulations. Additionally, components solubility in the medium and previous formulation treatments are also a decisive factor for nanoparticle formation. In particular, the treatment provided by hot-melt extrusion and FDM 3D printing affected the dissolution efficiency enhancing the interaction between the components, reverberating on particle size and particle formation kinetics mainly for HPMCAS and EUD RL. In conclusion, the 3D printing process influences the in-situ formation of nanoparticles, which can directly affect oral drug bioavailability and needs to be monitored.

FORMULATION AND IN-VITRO CHARACTERIZATION OF MUCOADHESIVE PATCHES OF ROOT EXTRACT OF ADENIUM OBESUM

Patches are punched from a sheet that serves as the intermediate product. Oral mucosal medication delivery alternatives to tablets have been studied, including polymers like cellulose etc. can be used to create mucosal patches. The present research was based on the development and in-vitro characterization of mucoadhesive patches of root extract of Adenium obesum utilizing different polymers. Adenium obesum (fresh roots) was obtained from the Unnao region. Eudragit L-100, Propylene glycol, Tween 80, Methanol, Ethanol and HPMCK 4M &amp; HPMCK 15M were purchased from the local market. The initial stages of processing involve grinding the roots into a coarse powder. The Soxhlet equipment was used to extract the powder and then weigh it. After preformulation study, the Adenium obesum mucoadhesive patches were created using the solvent casting technique. Patches were evaluated for physical appearances, thickness, pH, % drug content, in-vitro drug release, SEM and stability. In results, an excellent % drug release was demonstrated by the buccal patch. In order to estimate stability profile of mucoadhesive patches, it was evaluated for physical appearance. In conclusion, patches i.e., F2, F3 and F6 exhibited a significant estimation parameters like drug content, % drug release etc. The buccal drug of herbal (A. obesum) mucoadhesive patch has shown improved stability. It will ease to provide the long-lasting action by suppressing the symptoms of insomnia, agitations etc. Therefore, it may be produced commercially after its successful clinical trials.

Formulation and in vitro evaluation of compression coated mebeverine HCl tablets for colon targeting

The aim of the study was to develop colon targeted compression coated Mebeverine HCl (MEB) tablets using pH dependent, swellable and rupturable polymers for effective treatment of irritable bowel syndrome (IBS). The MEB loaded core tablets were prepared by direct compression method using CCM and CP as super disintegrating agents at different concentrations and evaluated for pre compression and post compression parameters. The optimized core tablets were further used to fabricate compression coated tablets using different ratios of Eudragit L100, Eudragit S100 as pH- dependent polymers, Keltone and Ethocel as swellable and rupturable polymers by modified compression method. Drug compatibility with excipients was checked by FTIR studies and results indicate no interaction. The precompression and post compression studies were within acceptable limits. In vitro dissolution studies were done for compression coated tablets to find out the lag phase, burst drug release and retard drug release The findings of this study concludes that the lag time of compression coated tablet can be modulated by combining with EL 100, ES 100, Keltone and Ethocel in different weight ratio. These designed tablet system was found to be satisfactory in terms of release of the drug after the predetermined lag time, thus the system can be target to release in the colon proximity. The compression coating technique can be successfully applied for MEB for colon targeting to treat IBS.

Developing sodium metabisulfite (SMBS)-containing Eudragit L100-55 microparticles for controlled intestinal release of SMBS to detoxify deoxynivalenol

This study aimed to achieve effective in vivo detoxification of deoxynivalenol (DON) contained in piglet feedstuff by developing sodium metabisulfite (SMBS)-containing Eudragit L100-55 (ES) microparticles as a novel feed additive. DON detoxification was assessed in vitro (IPEC-J2 cell) and in vivo (piglet). Within 2 h of exposure to simulated gastric fluid (SGF), 14.31% of encapsulated SMBS was released from ES microparticles, while 82.93% was released in another 80 min in simulated intestinal fluid (SIF). In IPEC-J2 cells, 0.1% ES microparticles remediated the toxicity of DON after 2 h incubation in SGF and 40 min in SIF. Forty weaned piglets with similar body weights (10 pigs/treatment) were fed for 28 days. Four diets were used: negative control (NC, 0.00 ppm DON), positive control (PC, 3.33 ppm DON), pure SMBS (PST, 3.33 ppm DON and 0.2% SMBS), and ES microparticles (EST, 3.33 ppm DON and 0.40% ES microparticles). The PC diet reduced ADG by 21.4% and ADFI by 20.1% compared to the NC diet (P < 0.05). The EST diet increased ADG and ADFI by 21.7% and 17.7% compared to the PC diet (P < 0.05), with no significant difference from the NC diet (P > 0.05). Compared to the PC and PST diets, the EST diet increased villus height, villus height/crypt depth ratio, mRNA levels of claudin 3 and peptide transporter 1, and decreased mRNA level of toll-like receptor 4 (P < 0.05). ES microparticles could protect SMBS, and the released SMBS could mitigate the toxic effects of DON in piglets.

Development and Characterization of Solid Dispersion of Rasagilline Mesylate for Improvement of Dissolution Rate Using Hydrophilic Carriers

The aim of present study was to improve the solubility of Rasagilline mesylate, an Atypical Antipsychotic agent which is BCS Class III drug and thus has very low solubility and hence very poor bioavailability owing to less absorption. Moreover Rasagilline mesylate has a bitter taste. Thus in the present study an attempt was made to taste mask the bitter taste of drug and improve oral bioavailability of drug by formulating the drug into solid dispersion and then formulate the solid dispersions into Fast Dissolving Tablets. Solid Dispersions of Rasagilline mesylate were formulated using various polymers like Plasdone K30, plasdone K90, Eudragit RS100, Eudragit RL 100, Poloxamer 188 and Soluplus in different ratios viz., 1:1 and 1:2 by solvent evaporation method and evaluated for various physicochemical parameters. On the basis of evaluation parameters Solid Dispersion containing Drug : Soluplus :: 1 : 2 was optimized batch having Solubility 1.91 mg/ml, Drug content 102.75 % and % CDR of 98.43 % at 35 mins. For formulating Fast Dissolving Tablets, 32 factorial designs was applied where the batch SD12 and Concentration of Chitosan were taken as dependent variable X1 and X2, respectively and wetting time (sec.) and in vitro disintegration time (sec.) and % CDR were taken as an independent variables. All the formulation prepared by applying experimental design showed more than 93 % drug release in 15 mins. Batch F9 was selected as an optimized batch from the data of overlay plot, drug release kinetics and checkpoint batch. A stability study for optimized formulation was carried out as per ICH guidelines, showed no significant changes in the evaluation parameters. Thus from the study it can be concluded that Fast Dissolving Tablets of Rasagilline mesylate formulated from solid dispersions can provide rapid drug release within a short period of time.

Formulation and Evaluation of Double-layered (Matrix and Drug-in-adhesive) Transdermal Patches of Diclofenac Diethylamine: In vitro and ex vivo Permeation Studies

Abstract: Background: The objective of this current study was to fabricate and characterize the sustained release double layered transdermal patches of Diclofenac Diethylamine using hydrophobic acrylic polymer Eudragit RL 100 and hydrophilic polymer Polyvinyl pyrrolidone K-30 in combination as first layer of matrix type patch and pressure sensitive acrylic adhesive Duro Tak 387- 2510 as the second layer of drug-in-adhesive type patch to provide sustained anti-inflammatory effect. Materials and Methods: Solvent casting method was employed to prepare patch over the backing membrane. The double layered technique were attempted to create the desirable features of acrylic polymer and adhesive. The drug-polymers compatibility studies were examined by Infrared spectroscopy. A full-thickness excised abdominal rat skin sample was used to perform the permeation studies using Franz’s Diffusion Cell. Results: Drug-polymers compatibility studies revealed no evidence of interaction and the formulations showed satisfactory physicochemical-mechanical characteristics. It was found that release profiles were affected by the proportion of polymer and permeation enhancer used. The optimized formulation MF3 showed maximum in vitro and ex vivo percent cumulative drug permeated i.e. 87.28 ± 3.88% and 81.95 ± 2.64% respectively, with flux 12.96 ± 0.51 μg/ cm2/h and permeability coefficient 1.09 ± 0.45 cm/h, in 24 hr. Also, the permeation studies suggested that dimethyl sulphoxide exhibit more promising results as permeation enhancer. Conclusion: It was concluded that an ideal Diclofenac Diethylamine double layered transdermal patch would serve as the best carrier to provide sustained effect with desirable permeation enhancement characteristics. Keywords: Transdermal patches, Double layered technique, Hydrophobic acrylic polymer, Hydrophilic polymer, Permeation enhancer, Anti-inflammatory.

Rationally designed nanoparticulate delivery approach for silymarin with natural bio-enhancer: In vitro characterization and in vivo evaluations of hepatoprotective effects in a mouse model

The proposed research study accentuates the delivery of drug and natural bioenhancer by utilizing a nano-platform based on eudragit RL (ERL) for enhanced efficacy, bioavailability, synergistic effect, and minimal toxic effects. ERL was utilized to encapsulate Silymarin and natural bioenhancer (Piperine) for rationally Box-Behnken design (BBD) based development of Silymarin-piperine nanoparticles (SL-P NPs) by nanoprecipitation method. The optimized SL-P NPs were 247.4 ± 4.5 nm in size, with 0.242 ± 0.002 PDI and 95.92 ± 1.01% entrapment efficiency, respectively. The surface morphology and shape were verified by SEM and TEM analysis. Differential scanning calorimetry demonstrated that the drug was successfully loaded into the NPs, and FTIR validated polymer and drug compatibility. In vitro release studies revealed cumulative drug release of 96.16 ± 2.87% in phosphate buffer saline (pH 7.4) for 24 h. We also evaluated the antioxidant mechanism of silymarin, adding to our understanding of SL-P NPs’ antioxidant characteristics as compared with Silymarin, Piperine, and Vitamin E. In vivo hepatoprotective evaluation of SL-P NPs in APAP-intoxicated mice portrayed significantly improved different biochemical parameters (p < 0.0001) as compared to the marketed product which was further confirmed by histopathological assessment of the liver. In conclusion, the co-delivery approach of silymarin with bioenhancer was proved to be beneficial and highly effective in enhancing bioavailability, solubility, and liver toxicity alleviation.