Development and Characterization of Eudragit-RL-100-Based Aceclofenac Sustained-Release Matrix Pellets Prepared via Extrusion/Spheronization

Aceclofenac (AC) is a nonsteroidal anti-inflammatory drug used in the treatment of chronic pain in conditions such as rheumatoid arthritis, with frequent administration during the day. The formulation of sustained release matrix pellets can provide a promising alternative dosage form that controls the release of the drug, with less blood fluctuation and side effects—especially those related to the gastric system. The extrusion/spheronization technique was used to formulate AC matrix pellets. The response surface methodology (version 17.2.02.; Statgraphics Centurion) was used to study the impacts of Eudragit RL 100 and PVP K90 binder solution concentrations on the pellets’ wet mass peak torque, pellet size, and the release of the drug. Statistically, a significant synergistic effect of PVP K90 concentration on the peak torque and pellet size was observed (p = 0.0156 and 0.031, respectively), while Eudragit RL 100 showed significant antagonistic effects (p = 0.042 and 0.013, respectively). The peak torque decreased from 0.513 ± 0.022 to 0.41 ± 0.021 when increasing the Eudragit RL 100 from 0 to 20%, and the pellet size decreased from 0.914 ± 0.047 to 0.789 ± 0.074 nm. The tested independent factors did not significantly affect the drug release in the acidic medium within 2 h, but these pellet formulae maintained the drug release at less than 10% in the acidic medium (pH 1.2), which may decrease gastric irritation side effects. In contrast, a highly significant synergistic effect of Eudragit and highly antagonistic effect of the PVP solution on drug release in the alkaline-pH medium were observed (p = 0.002 and 0.007, respectively). The optimized pellet formula derived from the statistical program, composed of 3.21% Eudragit and 5% PVP solution, showed peak torque of 0.861 ± 0.056 Nm and pellet size of 1090 ± 85 µm, and resulted in a significant retardation effect on the release after 8 h compared to the untreated drug.

Determination of Pickering Nanoemulsion by Eudragit Rl-100 Nanoparticle as Oral Drug Delivery for Poorly Soluble

Objective: The purpose of this research study was to develop Ketoprofen-loaded Pickering nanoemulsion with the help of polymeric nanoparticles [NPs]. The pickering nanoemulsion formulation is developed using Eudragit RL 100, which has the greater ability to stabilize the formulation as well as it better controls the release of drug upon oral administration. Method: In the present study, Ketoprofen - loaded Pickering nanoemulsion were prepared using an ultrasonic emulsification process. For the preparation of the Nanoemulsion, an aqueous phase of the nanodispersion of nanoparticle is used while Captex -300 and drug premix is used as oil phase. The nanoemulsion is formulated by using a probe sonicator with different ratios of aqueous phase and oil phase. The preformulation study of polymer or drug is done by FTIR and DSC and the drug - polymer compatibility was confirmed by FTIR. The prepared formulation was evaluated for physical appearance, pH, Viscosity, In vitro drug release, Particle size, Zeta Potential, Polydispersivity index, and transmission electron microscopy and stability. The Formulation is optimized for the different concentrations of the aqueous phase and oil phase with concentrations of drug and polymer. Results: All the prepared formulations show particle size in between 100-500nm hence it indicats formation of nanoemulsion. The zeta potential is -46mv which indicates good stability of formulation. The In vitro drug release shows maximum drug release i.e. 96.93% in 10 hrs which shows that the release of drug is prolonged due to formation of Polymer NPs. Conclusion: Thus the drug release was significantly controlled and slowed down when nanoemulsion is formulated by using NPs in comparison with control. These results fulfilled the objective of the study. This study opens new prospects on the formulation of Pickering nanoemulsion.

Dual-Acting Zeta-Potential-Changing Micelles for Optimal Mucus Diffusion and Enhanced Cellular Uptake after Oral Delivery

Context: Overcoming the intestinal mucosal barrier can be a challenge in drug delivery. Nanoemulsions with negative zeta potentials can effectively permeate the mucus layer, but those with positive zeta potentials are better taken up by cells; a nanoemulsion with capricious zeta potential from negative to positive can achieve both good permeation and high uptake. Objective: This study aimed to develop dual-acting zeta-potential-amphoteric micelles enabling optimal muco-permeation and enhancement of cellular uptake. Methods: A micellar pre-concentrate was prepared from 15% Labrasol, 15% Kolliphor EL, 30% Kolliphor RH 40, and 40% dimethylsulfoxide. The micellar pre-concentrate was loaded with anionic stearic acid (SA), forming ionic complexes with cationic polymers at a ratio of 25:1 with Eudragit RS 100 and Eudragit RL 100. Blank micelles and those containing complexes were separately diluted in physiological buffers and examined for their droplet sizes, polydispersity indices (PDIs), zeta potentials, and cytotoxicity. The SA release from the micellar complexes was evaluated in 0.1 mM phosphate buffer (pH 6.8) containing 0.001% fluorescein, thereby enabling an instant decrease in fluorescence. Finally, the micelles were loaded with the model drug fluorescein diacetate (FDA) and evaluated for their muco-permeation behavior and cellular uptake. Results: The micellar dilutions formed micelles at the critical micelle concentration (CMC) of 312 µg/mL and showed a uniform average droplet size of 14.2 nm, with a PDI < 0.1. Micellar dilutions were non-cytotoxic when used at 1:100 in a physiological medium. Micelles loaded with ionic complexes achieved a sustained release of 95.5 ± 3.7% of the SA in 180 min. Moreover, the zeta potential of the complex-loaded micelles shifted from −5.4 to +1.8 mV, whereas the blank micelles showed a stabilized zeta potential of −10 mV. Furthermore, the negatively charged blank and complex-loaded micelles exhibited comparable muco-permeation, with an overall average of 58.2 ± 3.7% diffusion of FDA. The complex-loaded micellar droplets, however, provided a significantly higher cellular uptake of the model drug FDA (2.2-fold, p ≤ 0.01) Conclusion: Due to undergoing a shift in zeta potential, the modified micelles significantly enhanced cellular uptake while preserving mucus-permeating properties.

Formulation and Invitro Characterization of Fluvoxamine Loaded Nanoparticles

Fluvoxamine is an antidepressant that functions pharmacologically as a selective serotonin reuptake inhibitor. Though it is in the same class as other SSRI drugs, it is most often used to treat obsessive-compulsive disorder. As the biological half-life of the drug is 15.6 hrs and belongs to BCS class II. To overcome these problems, Nanoparticles of Fluvoxamine were formulated by using Ethyl Cellulose, Eudragit RS 100 & Eudragit Rl 100 as a polymer by emulsification method. Among all the 9 formulations F6 formulation is optimized, as it shows maximum drug release at the end of 12hrs which suits the controlled release drug delivery system criteria as per our studies, having acceptable particle size, SEM, and Zeta potential value. From the drug release kinetics of the F8 formulation of Losartan Nanoparticles dispersion, it was concluded that the F8 formulation follows Zero-order drug release with super case II transport mechanism.

Design and Development of Transdermal Patches of Antipsychotic Drug: In vitro and Ex vivo Characterization

The purpose of the present research work was to design, assess, and estimate the developed transdermal matrix-type formulation comprising levosulpiride hydrochloride with the objective of enhancing the bioavailability and compliance of the patient. Transdermal films of levosulpiride were developed using a solvent casting method by hydroxypropyl methylcellulose (HPMC) E 15, Eudragit RL 100, and Eudragit RS100. In current research work, propylene glycol and oleic acid was used as plasticizer and permeation enhancers in different fractions. Among the batches, drug content uniformity with all formulations was perceived between 91.6 to 98%. Folding endurance of patches was good and indicates satisfactory flexibility. Developed transdermal films had the necessary physicochemical properties, for example, uniformity of drug content, weight, thickness, folding endurance, and dampness content. Franz diffusion cell was used for in vitro diffusion studies utilizing dialysis membrane as a pervasion boundary. Formulation F5 (Eudragit RL 100-1%, HPMC E15-9%) was found to be best among all batches of its consistent release rate for 12 hours and the extent of drug release 97.76%. F5 was the most palatable formulation as it firmly meets the standards and continuously permeated drugs for 12 hours that can keep up desired therapeutic concentration in plasma. The patches were exposed to transient stability studies and were observed to be constant and stable.

Impact Of Defensive Covering Of Anti-Inflamatory Medicine Tablets With Acrylatemethacrylate Copolymers On Tablet Crumbling Times And Disintegration Rates

Tablets of headache medicine (a dampness degradable medication) have been film covered with two undifferentiated from Eudragit RL and RS copolymers assigned here as An and B which vary just in their cation content in the proportion 2:1 (A:B). An, is in this manner more hydrophilic than B. The tablets were film covered with ethanol arrangements of these two polymers. Film covering with either An or B fundamentally decreased the dampness take-up possibilities of the tablets however caused an expansion in the breaking down occasions of the tablets and hindered disintegration rates. The mean deterioration times were 0.5±0.1 min (uncoated tablets), 16±2.5 min (tablets covered with An) and 115±3.6 min (tablets covered with B). The relating disintegration rates % h - 1 were 28.3 for uncoated, 16.6, covered with An and 14.8, covered with B, separately. Subsequently, covering with polymer B impressively impeded the crumbling and disintegration properties of the tablets.

Formulation and Evaluation of Eudragit RL-100 Nanoparticles Loaded In-Situ Forming Gel for Intranasal Delivery of Rivastigmine

Purpose: Rivastigmine hydrogen tartrate (RHT) is commonly used for the treatment of mild to moderate Alzheimer’s disease (AD). The aim of this work was to formulate in-situ pluronic F-127 (PF-127) hydrogels containing Eudragit RL-100 (EU-RL) nanoparticles (NPs) in order to improve the therapeutic efficacy of RHT through the nasal route. Methods: The NPs were prepared using different polymer to drug ratios and evaluated for their physicochemical characteristics, cellular uptake and in vitro cytotoxicity against lung adenocarcinoma cells (A459). PF-127 nanoformulations were prepared via cold method and analyzed in terms of physicochemical properties and drug release profiles. The nanoformulations and plain drug gel were then assessed by ex vivo permeation studies across the sheep nasal mucosa. Results: The EU-RL NPs exhibited a particle size within the range of 118 to 154 nm and positive zeta potential values of 22.5 to 30 mV with an approximately spherical shape. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD) suggested no drug to polymer interaction through the preparation of nanoformulations. The RHT-loaded NPs exhibited an acceptable cytocompatibility with a time- and dose-dependent cellular internalization. Conclusion: Our results clearly indicated the potential of nanoformulations as controlled release systems to improve the therapeutic efficacy of RHT through the intranasal administration

Design, development and characterization of ketorolac tromethamine polymeric nanosuspension

Aim: At present, various ophthalmic formulations show low bioavailability. The rationale of present work was to design and develop stable ketorolac tromethamine nanosuspension with sustained effect and greater permeability for ocular drug delivery and increased ocular residence. Materials & methods: Formulations were designed by using central composite design, developed by combined nanoprecipitation and probe sonication method. Results & discussion: Nanosuspensions depicted the size range of the particles in between 199 and 441 nm with slight reduction in crystallinity of drug. In vitro drug release revealed that higher % entrapment efficiency of drug in nanosuspension delays the drug release. Conclusion: Eudragit RL-100-based nanosuspension increases viscosity and avoids problems like drug loss from precorneal surface and rapid drainage through nasolacrimal areas.