Formulation of Microwave-Assisted Natural-Synthetic Polymer Composite Film and Its Physicochemical Characterization

This study is aimed at microwave-assisted synthesis of sodium carboxymethylcellulose and Eudragit L100 composite film and its physicochemical characterization. The film was developed with varying quantities of each polymer and treated with microwave at a fixed frequency of 2450 MHz with a power of 350 Watts for 60 and 120 s. All formulations were characterized for thickness/weight uniformity, moisture adsorption, erosion and water uptake, tensile strength, and vibrational, thermal, and surface morphological analysis in comparison with untreated film samples. Results indicated that microwave treatment for 60 s significantly improved the tensile strength, reduced the water adsorption, delayed erosion, and reduced the water uptake in comparison with the untreated and 120 s treated film formulations. The vibrational analysis revealed rigidification of hydrophilic domains at OH/NH moiety and fluidization of hydrophobic domains at asymmetric and symmetric CH moieties, which is envisaged to be due to the formation of new linkages between the two polymers. These were later confirmed by thermal analysis where a significant rise in transition temperature, as well as enthalpy of the system, was recorded. The microwave treatment for 60 s is thus advocated to be the best treatment condition for developing sodium carboxymethylcellulose and Eudragit L100 composite polymeric films.

Hybrid Nanoparticles for Haloperidol Encapsulation: Quid Est Optimum?

The choice of drug delivery carrier is of paramount importance for the fate of a drug in a human body. In this study, we have prepared the hybrid nanoparticles composed of FDA-approved Eudragit L100-55 copolymer and polymeric surfactant Brij98 to load haloperidol—an antipsychotic hydrophobic drug used to treat schizophrenia and many other disorders. This platform shows good drug-loading efficiency and stability in comparison to the widely applied platforms of mesoporous silica (MSN) and a metal–organic framework (MOF). ZIF8, a biocompatible MOF, failed to encapsulate haloperidol, whereas MSN only showed limited encapsulation ability. Isothermal titration calorimetry showed that haloperidol has low binding with the surface of ZIF8 and MSN in comparison to Eudragit L100-55/Brij98, thus elucidating the striking difference in haloperidol loading. With further optimization, the haloperidol loading efficiency could reach up to 40% in the hybrid Eudragit L100-55/Brij98 nanoparticles with high stability over several months. Differential scanning calorimetry studies indicate that the encapsulated haloperidol stays in an amorphous state inside the Eudragit L100-55/Brij98 nanoparticles. Using a catalepsy and open field animal tests, we proved the prolongation of haloperidol release in vivo, resulting in later onset of action compared to the free drug.

Interpolymer Complex of Chitosan and Eudragit L-100: Preparation, Characterization and Drug Release Behavior

Aims: The aim of the present investigation was to prepare interpolymer complex between Chitosan and Eudragit L100, and to evaluate its performance as a matrix for controlled release of drugs, using Diclofenac sodium as a model. Methodology: Interpolymer complex were prepared by combining different % chitosan solutions with different % Eudragit L100 solutions in different ratios. The formation of interpolyelectrolyte complexes (IPEC) between carbopol and Chitosan was investigated, using turbidimetry and viscosity measurement. The structure of the prepared IPEC was investigated using FTIR spectroscopy and DSC. A Rotary compression press was used to formulate matrix tablets of diclofenac sodium using polymers in physical mixture and IPECs.The amount of Diclofenac Sodium released in the dissolution medium was determined spectrophotometrically at 276 nm. Results: The results of the present investigation confirmed the formation of an interpolyelectrolyte complex between Chitosan and Eudragit L 100. The release of the model drug Diclofenac sodium was significantly controlled from tablets made up of the IPEC as compared with polymers alone and in combination. Release profiles were represented by a mathematical model, which indicates that the prepared system releases drug in a zero-order manner by changing the ratio of the IPEC in the tablets. Conclusion: Controlled release drug delivery systems designed to manipulate the drug release to achieve specific clinical objectives that are unattainable with conventional dosage forms.

Vaginal delivery of clotrimazole by mucoadhesion for treatment of candidiasis

The aim of this study was to prepare mucoadhesive vaginal tablets of clotrimazole for treatment of vaginal candidiasis. A combination of mucoadhesive polymers like HPMC K100M, Sodium CMC, and Eudragit L100 were used in different ratios prepare solid dispersions to enhance its solubility. Tablets were prepared by the wet granulation method. Solid dispersions were evaluated for saturation solubility. All tablet batches were evaluated for weight variation, hardness, friability, drug content, swelling index, in vitro drug release study, ex vivo diffusion and mucoadhesive strength. FTIR spectra showed there was no interaction between the drug and the excipients. HPMC K100 M increased the solubility of clotrimazole in simulated vaginal fluid at pH 4.5. Eudragit L100 was shown to increase the swelling and mucoadhesive strength of the tablet, i.e., 3.03 and 3.29 g. The in vitro and ex vivo release of all 9 batches showed between 61 to 78% release in 8h. Ex vivo diffusion studies using sheep vaginal membrane showed 43 to 59% in 6h in simulated vaginal fluid. The release and flux were nearly comparable to marketed tablet i.e., Candid-V6. The drug release of all batches followed the Korsmeyer-Peppas kinetic model, and the mechanism was found to be non‐Fickian/anomalous. Keywords: Clotrimazole, solid dispersion, HPMC K100M, Eudragit L100, Sodium CMC.

PSIII-21 Efficacy of deoxynivalenol detoxification by sodium metabisulfite (SMBS) containing nanofibrous mats using an in vitro intestinal epithelial cell IPEC-J2

Deoxynivalenol (DON) occurs in many commonly used cereal grains. Pigs feed with DON concentrations as low as 0.6–2.0 mg/kg can result in reduced feed intake and growth rate, damage to intestinal epithelial cells, and increase susceptibility to enteric pathogens. Sodium metabisulfite (SMBS) can efficiently detoxify DON by converting it 8-DONS or 10-DONS in vitro. However, if SMBS is added directly to the feed, SMBS rapidly degrades under acidic aqueous conditions (e.g. pig stomach) and little SMBS is delivered to the intestinal absorption site where it can effectively detoxify DON. Thus, the objective of this study was to encapsulate SMBS into Eudragit L100-55 nanofibrous mats to deliver intact SMBS to the small intestine and evaluate the efficacy of DON detoxification in the simulated intestine fluid (SIF) using an in vitro intestinal epithelial cell (IPEC-J2) model. Nanofibrous mats were produced by coaxial electrospinning, with peak loading capacity and loading efficiency of SMBS reaching 32.00% and 80.01%. DON-induced cytotoxicity was not observed during in vitro analysis consisting of incubation of DON in the presence of SMBS-containing nanofibers (0.5% w/w) in simulated gastric fluid (SGF) for 2 h followed by incubation in a mixture of SGF and SIF (1:1) for 20 min. Meanwhile, compared to the DON treatment, incubation of DON in the presence of SMBS-containing nanofiber (0.5% w/w) in SGF for 2 h and SIF for 20 min decreased the gene expression of inflammatory cytokines in the IPEC-J2 cells and maintained the cell integrity. To conclude, SMBS released from Eudragit L100-55 nanofibrous mats in the SIF effectively decreased the adverse effects induced by DON in the IPEC-J2 cells. Nanofibrous mats can release a large amount of SMBS in a short time in SIF to achieve the effect of detoxifying DON.

A Novel Pulsatile Release Film Coated Tablet of Zaltoprofen Loaded SNEDDS

The aim of the present study was to formulate pulsatile release film coated tablet of zaltoprofen for the treatment of rheumatoid arthritis. Initially solubility of zaltoprofen was enhanced by formulating self emulsifying fast disintegrating tablet of zaltoprofen. Core fast disintegrating tablet of zaltoprofen was coated with ethyl cellulose and eudragit L100 in various proportions as coating polymer. Ethanol was used as coating solvent and dibutyl phthalate as plasticizer. Film coated tablet with different coating levels were formulated and were evaluated for parameters like lag time, rupture time, in vitro dissolution etc. Amongst the nine different formulations P-4 formulation containing 3:1 ratio of ethyl cellulose and eudragit L100 with 5% coating level gives desired lag time with best drug dissolution profile. Formulated film coated tablet of zaltoprofen can be useful for chronotherapeutic treatment of rheumatoid arthritis.

Formulation of Extended-Release Ranolazine Tablet and Investigation Its Stability in the Accelerated Stability Condition At 40⁰C And 75 % Humidity

Formulation of Ranolazine in the form of extended-release tablet in 500 mg dosage form was performed using Eudragit L100-55 as a retarding agent. Drugrelease profiles were investigated in comparison with the reference Ranexa extended-release 500 mg tablet. F2 and f1 were calculated as 64.16 and 8.53, respectively. According to Peppas equation, the release of drug is controlled by diffusion (n=0.5). The tablets were put into accelerated stability condition (40⁰C, 75% humidity) for 3 and 6 months. The dissolution release profiles and other physical and chemical characteristics of the tablets confirmed the robustness and stability of formulation in this condition.