Improving the solubility of nevirapine using a hydrotropy
and mixed hydrotropy based solid dispersion approach

Madan, Jyotsana; Kamate, Virendra J.; Dua, Kamal; Awasthi, Rajendra

doi:10.17219/pim/77093

Cited by 11 publications

(4 citation statements)

References 19 publications

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“…DSC runs were performed from 30 to 300°C at the 10°C/min heating rate. An empty aluminium pan was utilized as a reference material to calibrate the DSC temperature scale and enthalpic response [ 32 ]. Nitrogen was used as a purge gas, flowing through the apparatus at 20 cm 3 min −1 .…”

Section: Methodsmentioning

confidence: 99%

Solid Dispersion Pellets: An Efficient Pharmaceutical Approach to Enrich the Solubility and Dissolution Rate of Deferasirox

Farmoudeh

Rezaeiroshan

Abbaspour

et al. 2020

BioMed Research International

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Deferasirox (DFX) is an oral iron-chelating agent and classified into class II of the Biopharmaceutics Classification System. Low bioavailability of the drug due to insufficient solubility in physiological fluids is the main drawback of DFX. The idea of the current study was to explore the potential of solid dispersion (SD) as an effective method to improve the dissolution rate of DFX in pellets. The SDs were made by the solvent evaporation technique using polyethylene glycol 4000 (PEG 4000) and polyvinylpyrrolidone K25 with different drug-to-carrier ratios. Then, the dispersion was milled and mixed with other components and the mixture layered on sugar-based cores by pan coating technique. The pellets were evaluated in terms of size distribution, morphology (SEM), and dissolution behaviour. Drug-polymer interactions were studied using differential scanning calorimetry (DSC), X-ray diffraction study (XRD), and Fourier transformation infrared (FTIR) spectroscopy. The pellets coated with SD showed a remarkable rise in the solubility of DFX than that of free drug-loaded pellets. The dispersion with PVP K25 showed a faster dissolution rate as compared to other mixtures. The DSC and XRD analysis indicated that the drug was in the amorphous state when dispersed in the polymer. The FTIR studies demonstrated any ruled out interaction between drug and polymer. The SEM showed smoothness on the surface of the pellets. It is resolved that the SD method considerably enriched the dissolution rate of DFX in pellets, which can also be utilized for other poorly water-soluble drugs.

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Section: Methodsmentioning

confidence: 99%

Solid Dispersion Pellets: An Efficient Pharmaceutical Approach to Enrich the Solubility and Dissolution Rate of Deferasirox

Farmoudeh

Rezaeiroshan

Abbaspour

et al. 2020

BioMed Research International

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“…The results of the solubility test on S1, S2 and S3 observed in distilled water were 0.485, 0.2186, 0.1748 respectively as shown in table 3. It was noted that the solubility of the prepared solid dispersion decreased as the ratio of carrier increases [35][36][37].…”

Section: Determination Of Solubility Of Solid Dispersionmentioning

confidence: 99%

Solubility Enhancement of Diclofenac Using Solid Dispersions

Mirza¹

2021

Int J Pharm Pharmacol

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Background: The phenomenon which gives rise to a homogenous system, formed by the dissolution of solute in a solvent is known as solubility. Low solubility is the limiting factor in formulation development. Diclofenac being BCS class II drug have low aqueous solubility of 0.00401mg/ml. Amongst various solubility enhancement techniques, solid dispersion is the easiest one. Objective: Present work is primarily focused on the development of solid dispersions of diclofenac through solvent evaporation technique utilizing Eudragit E100 as a carrier. Methods: Solid dispersion consists of at least one active pharmaceutical ingredient as a carrier in solid state. Various methods for preparing solid dispersions includes melt extrusion, fusion lyophilization, spray drying, solvent evaporation, and super critical fluid (SCF) technology. Solvent evaporation technique is used among various solid dispersion methods. Conclusion: The enhanced solubility found to be 0.485mg/ml. The dissolution was performed using USP Type II apparatus was %CDR of pure drug and its solid dispersion in 8 hr were found out to be 45.14926% and 98.04758% respectively. Henceforth, solid dispersion technique results marked solubility enhancement of diclofenac sodium.

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“…41 and the CLXB concentration was determined using UV-visible spectrophotometer (JascoV-730, Tokyo, Japan) at 254 nm. 18…”

Section: Solubility Studiesmentioning

confidence: 99%

Formulation and In Vitro Evaluation of Casein Nanoparticles as Carrier for Celecoxib

et al. 2020

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Purpose : The objective of this work was to formulate casein (CAS) nanocarriers for the dissolution enhancement of poorly water soluble drug celecoxib (CLXB). Methods: The CLXB loaded CAS nanocarriers viz., nanoparticles, reassembled CAS micelles and nanocapsules were prepared using sodium caseinate (SOD-CAS) as a carrier to enhance the solubility of CLXB. The prepared formulations were characterized for particle size, polydispersity index, zeta potential, percentage entrapment efficiency, and surface morphology for the selection of best formulation. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray powder diffraction study was used to for the confirmation of encapsulation of CLXB. Further, in vitro drug dissolution, ex-vivo permeation studies on chicken ileum and stability studies were carried out. Results: The CLXB loaded casein nanoparticles (CNP) (batch A2) showed a particle size diameter 216.1 nm, polydispersity index 0.422 with percentage entrapment efficiency of 90.71% and zeta potential of -24.6 mV. Scanning electron microscopy of suspension confirmed globular shape of CNP. The in vitro release data of optimized batch followed non Fickian diffusion mechanism. The ex vivo permeation studies on chicken ileum of CLXB loaded CNP showed permeation through mucous membrane as compared to pure CLXB. The apparent permeability of best selected freeze dried CLXB loaded CNP (batch A2) was higher and gradually increased from 0.90 mg/cm2 after 10 min to a maximum of 1.95 mg/cm2 over the subsequent 90 min. A higher permeation was recorded at each time point than that of the pure CLXB. Conclusion: The study explored the potential of CAS as a carrier for solubility enhancement of poorly water soluble drugs.

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Improving the solubility of nevirapine using a hydrotropy and mixed hydrotropy based solid dispersion approach

Cited by 11 publications

References 19 publications

Solid Dispersion Pellets: An Efficient Pharmaceutical Approach to Enrich the Solubility and Dissolution Rate of Deferasirox

Solid Dispersion Pellets: An Efficient Pharmaceutical Approach to Enrich the Solubility and Dissolution Rate of Deferasirox

Solubility Enhancement of Diclofenac Using Solid Dispersions

Formulation and In Vitro Evaluation of Casein Nanoparticles as Carrier for Celecoxib

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