Etodolac (ETD) is a non-steroidal anti-inflammatory drug (NSAID) given in rheumatoid arthritis treatment. As it comes under BCS class II drug hence it exhibits low water solubility. Also, its dissolution rate-limited oral absorption results in delayed onset of action. The Novel approach in the solubility enhancement field; crystal engineering was preferred to prepare pharmaceutical cocrystals of etodolac with GRAS (generally recognized as safe) molecules. Pharmaceutical cocrystals of etodolac were prepared with p-hydroxybenzoic acid and glutaric acid with the drug: coformer ratio 1:1 and 1:2. Cooling cocrystallization was used to prepare etodolac cocrystals. Cocrystal formulations were characterized by saturation solubility study, in-vitro dissolution studies, and stability study. Cocrystal was also characterized by analytical parameters like Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). Optimized Cocrystal formulation dissolved more rapidly and their equilibrium solubility is greater than the plain drug.
Introduction: Etodolac is used in the treatment of acute pain and inflammation. It has low solubility because of high hydrophobicity and it is reported that upon oral administration shows gastric disturbances. This encourages the development of topical vesicular formulation.
Method: In this work we used coacervation-phase separation method for the development of etodolac loaded vesicular system by using non-ionic surfactants, cholesterol and soya lecithin. Central composite design (rotatble) was used to optimize the concentrations of soy lecithin, surfactant and cholesterol. The prepared formulations were characterized by number of vesicles formed, vesicle size, zeta potential, entrapment efficiency, in-vitro permeation, ex-vivo permeation and anti-inflammatory study.
Results: Etodolac was successfully entrapped in all formulations having efficiency in the range of 74.36% to 90.85%, which was more at 4 °C than room temperature. When hydrated with water; niosome in the range of 54 to 141 (per cubic mm) were spontaneously produced. The results of in-vitro diffusion study revealed that etodolac was released in the range of 71.86 to 97.16% over a period of 24 hrs. The average vesicle size of optimized formulation was found 211.9 nm with PDI of 0.5. The observed responses i.e. % encapsulation efficiency and drug release were 74.12 and 95.08 respectively. The zeta potential was -19.4mV revealed the stability of formulation which was further confirmed by no changes in drug content and drug release after stability studies. The % inhibition in paw volume was 40.52% and 43.61% for test and marketed proniosomal gel.
Conclusion: Proniosomal gel formulation was stable and could enhance skin delivery of etodolac because of excellent permeation capability of vesicular system.
Objectives: Chemotherapy has various side effects and toxins, to overcome these problems nanoparticles are formed. Nanoparticles accumulate in tumor cells due to EPR effect. Given the role of P-gp in influencing drug’s pharmacology, methods to overcome P-gp mediated efflux have been investigated. The objectives of present research were to formulate nanoparticles containing DOX and PTX. The present research also includes the potential of flavonoids such as silymarin (SLM) to act as P-gp inhibitors, enabling increased absorption and inhibition of excretion and modulation of multi-drug resistance.
Materials and Methods: Nanoparticles of PLGA and BSA were developed paclitaxel (PTX). Using 23 factorial designs total eight formulations of PTX-PLGA and PTX-BSA nanoparticles were prepared. PLGA (A,) poly vinyl alcohol (PVA) (B) and speed (C) used as independent variants in size of the particles (Y1), efficiency of entrapment (Y2) and % release of drug (Y3) taken as a dependent variable. PTX was successfully applied to the micelles by dissolving.
Results: The median diameter of PTX-BSA and PTX-PLGA nanoparticles ranged from 104 to 1150 nm and 110 to 1023 nm respectively. The effectiveness of the entrapment and release of in vitro drugs also rely on the solubility of the drug and the polymer in the solvent. The use of software is a systematic tool for optimization, and it helps to reduce the cost of experiments.
Conclusion: From the experiments it was concluded that the prepared formulation helped to overcome the multiple drug resistance by incorporation of P-gp inhibitor like silymarin.
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