Incorporation of poorly soluble drug Cefixime inside the micellar core of conventional and gemini surfactants

This work reports the physicochemical behavior of antibiotic drug, cefixime (CEF) in presence of cetyl trimethyl ammonium bromide (CTAB), dodecyl trimethyl ammonium bromide (DTAB), dodecyl ethyl dimethyl ammonium bromide, (DDAB),...

Microfluidic Synthesis of Indomethacin-Loaded PLGA Microparticles Optimized by Machine Learning

Several attempts have been made to encapsulate indomethacin (IND), to control its sustained release and reduce its side effects. To develop a successful formulation, drug release from a polymeric matrix and subsequent biodegradation need to be achieved. In this study, we focus on combining microfluidic and artificial intelligence (AI) technologies, alongside using biomaterials, to generate drug-loaded polymeric microparticles (MPs). Our strategy is based on using Poly (D,L-lactide-co-glycolide) (PLGA) as a biodegradable polymer for the generation of a controlled drug delivery vehicle, with IND as an example of a poorly soluble drug, a 3D flow focusing microfluidic chip as a simple device synthesis particle, and machine learning using artificial neural networks (ANNs) as an in silico tool to generate and predict size-tunable PLGA MPs. The influence of different polymer concentrations and the flow rates of dispersed and continuous phases on PLGA droplet size prediction in a microfluidic platform were assessed. Subsequently, the developed ANN model was utilized as a quick guide to generate PLGA MPs at a desired size. After conditions optimization, IND-loaded PLGA MPs were produced, and showed larger droplet sizes than blank MPs. Further, the proposed microfluidic system is capable of producing monodisperse particles with a well-controllable shape and size. IND-loaded-PLGA MPs exhibited acceptable drug loading and encapsulation efficiency (7.79 and 62.35%, respectively) and showed sustained release, reaching approximately 80% within 9 days. Hence, combining modern technologies of machine learning and microfluidics with biomaterials can be applied to many pharmaceutical applications, as a quick, low cost, and reproducible strategy.

Effect Of Surfactant Chain Length On Emulsification Dynamics Of Self Emulsifying Formulation Of Poorly Soluble Drug

Aim: In this work the aim was to study the chain length of surfactant on the self emulsifying system of a poorly soluble drug, aceclofenac. The selection of almond oil as a lipid vehicle was done on basis of solubility and compatibility of the vehicle with the drug. Methods: The effect of varying chain length of different surfactants of Tween series namely Tween 20, Tween 40, Tween 60 and Tween 80 was evaluated on self emulsifying efficiency by constructing pseudoternary diagrams. PEG-400 was used as co-surfactant in a definite ratio with all the surfactants to minimize their concentration. The best self emulsifying ability was exhibited by Tween 80: PEG-400 combination followed by Tween 60: PEG-400, Tween 40: PEG-400, Tween 20: PEG-400. This observation indicates that as the chain length of Tweens increases their ability to form a good microemulsion increases if same co-surfactant is used. Results: However it has also been found that the presence of unsaturated bond in Tween 80 provides it an elasticity which supports good intermixing of oil and water and leading to formation of a fine microemulsion. Six different formulations were prepared using combination of almond oil, Tween 80, PEG-400 and the drug aceclofenac. Conclusion : The formulations were subjected to various evaluation parameters such as dispersibility, transmittance, pH, globule size, polydispersibility, zeta potential, viscosity, refractive index and in vitro dissolution. The best formulation was found to have globule size of less than 100 nm, zeta potential of -3.35 ± 0.60 mV which indicates formation of a microemulsion of aceclofenac with good stability.

Enhancement of Solubility and Dissolution Rate of BCS Class-II Fluvoxamine Tablets using Solvent Evaporation Solid Dispersion Technique

Aim: This research work was aimed to formulate Enhancing the solubility of Poorly soluble drug i.e. Fluvoxamine tablets by the solvent evaporation method, Fluvoxamine medicament is a selective serotonin reuptake inhibitor (SSRI) antidepressant agent. Purpose: The BCS class II drug Fluvoxamine consist low aqueous solubility and low oral bioavailability, for this reason to improve the biological performance of Fluvoxamine drug by solid dispersion mechanism. Methodolgy: The drug Fluvoxamine was formulated by using solvent evaporation technique, solid dispersions of Fluvoxamine were prepared with different carriers in different ratios of PEG 6000 & Mannitol (1:1, 1:2 and 1:3). Results: Results of prepared solid dispersions of Fluvoxamine by solid dispersion method Finally by comparing all the formulations, formulation (SF3) containing Fluvoxamine and PEG 6000 (1:3) shows better results. Conclusion: Here we concluded that the poorly soluble drug solubility improving by solvent evaporation solid dispersion mechanism, and also developed six Fluvovamine formulations (FDF1-FDF6) during this FDF4 shows maximum (98.9±0.8%) drug release at the end of time.

Formulation and Evaluation of Fast Dissolving Buccal Film of Curcumin as Promising Route of Buccal Delivery

The present work is mainly focused on preparing fast dissolving buccal films of Curcumin solid dispersion, since Curcumin is a poorly soluble drug. The main aim of this is to provide quick onset of action, improved bioavailability and also to increase the patient convenience of administration. The rate of dissolution can be increased by incorporating the solid dispersed drug into film which is prepared by HPMC-K100 as polymers, glycerin as a plasticizer, sorbitol as an antioxidant, Tween & Span as a non-ionic surfactant. The films were evaluated for their physiochemical parameters like disintegration time, surface pH, thickness, weight, percent moisture absorption, folding endurance, drug content and stability testing. The invention is to produce mucoadhesive buccal patches, which heals the lesion/ injury with replacing patches.

APPLICATION OF LIQUISOLID TECHNIQUE FOR ENHANCEMENT OF DISSOLUTION OF WATER INSOLUBLE DRUG CHOLECALCIFEROL

The issue of low solubility and bioavailability poses a significant challenge for most of the drug candidates for oral delivery. Liquisolid, a recently evolved technique for dissolution enhancement, can dodge these barriers. The purpose of this research was to increase the solubility of poorly soluble drug cholecalciferol by liquisolid technique. The cholecalciferol’s solubility studies were performed in a mixture of Polysorbate 80 and PEG 400 in different ratios (1:1, 1:2, 2:1, 1:3, and 3:1). Maximum solubility was observed in a 1:2 ratio. There were changes in the X-ray diffractogram and shifting of the endothermic peak in DSC from 85oC to 146oC, which indicated the drug’s conversion into an amorphous form. The liquisolid form was adsorbed on the carrier material and compressed. The optimization was done by using Plackett Burman Design with Design-Expert software. It was observed that the drugs release profile of the optimized formulation was better than the generic product and was comparable to Divisun tablets 2000 I.U (Innovator).