Improvement of solubility, dissolution and stability profile of artemether solid dispersions and self emulsified solid dispersions by solvent evaporation method

Ansari, Muhammad Tayyab; Arshad, Muhammad Sohail; Hussain, Altaf; Ahmad, Zeeshan

doi:10.1080/10837450.2016.1265554

Cited by 14 publications

(3 citation statements)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Various approaches have been employed to try and improve the solubility and thus anti-malarial activity of both of the components in Coartem® including nanostructured lipid carriers, self-emulsified solid dispersions, solid lipid microparticles and nanoemulsions ( Agbo et al, 2016 ; Laxmi et al, 2015 ; Parashar et al, 2016 ; Tayyab Ansari et al, 2016 ). Recently, it was demonstrated that lumefantrine amorphous solid dispersions improved its oral absorption relative to the crystalline reference ( Jain et al, 2017 ).…”

Section: Introductionmentioning

confidence: 99%

Physical stability and release properties of lumefantrine amorphous solid dispersion granules prepared by a simple solvent evaporation approach

Trasi

Bhujbal

Zemlyanov

et al. 2020

International Journal of Pharmaceutics: X

View full text Add to dashboard Cite

Amorphous solid dispersions (ASDs) of lumefantrine, which has low aqueous solubility, have been shown to improve bioavailability relative to crystalline formulations. Herein, the crystallization tendency and release properties of a variety of lumefantrine ASD granules, formed on a blend of microcrystalline cellulose and anhydrous lactose, prepared using a simple solvent evaporation method, were evaluated. Several polymers, a majority of which contained acidic moieties, and different drug loadings were assessed. Crystallinity as a function of time following exposure to stress storage conditions of 40 °C and 75% relative humidity was monitored for the various dispersions. Release testing was performed and ASD characteristics were further evaluated using infrared and X-ray photoelectron spectroscopy (XPS). A large difference in stability to crystallization was observed between the various ASDs, most notably depending on polymer chemistry. This could be largely rationalized based on the extent of drug-polymer interactions, specifically the degree of lumefantrine-polymer salt formation, which could be readily assessed with XPS spectroscopy. Lumefantrine release from the ASDs also varied considerably, whereby the best polymer for promoting physical stability did not lead to the highest extent of drug release. Several formulations led to concentrations above the amorphous solubility of lumefantrine, with the formation of nano-sized drug-rich aggregates. A balance between the ability of a given polymer to promote physical stability and drug release may need to be sought.

show abstract

Section: Introductionmentioning

confidence: 99%

Physical stability and release properties of lumefantrine amorphous solid dispersion granules prepared by a simple solvent evaporation approach

Trasi

Bhujbal

Zemlyanov

et al. 2020

International Journal of Pharmaceutics: X

View full text Add to dashboard Cite

show abstract

“…Amorphous solid dispersions present a promising strategy for improving the bioavailability of poorly soluble drugs [ 30 , 31 , 32 ]. Solid dispersions can be prepared by thermal methods (e.g., melting and hot-melt extrusion (HME)) [ 33 , 34 , 35 ], solvent evaporation [ 36 , 37 ], and supercritical fluid technology [ 38 , 39 , 40 ]. Binary solid dispersions of highly lipophilic drugs such as atovaquone and polymeric carriers are limited in their drug loading capacity and therefore their feasibility due to dissolution rate limitations [ 41 ].…”

Section: Introductionmentioning

confidence: 99%

A Repurposed Drug for Brain Cancer: Enhanced Atovaquone Amorphous Solid Dispersion by Combining a Spontaneously Emulsifying Component with a Polymer Carrier

et al. 2018

View full text Add to dashboard Cite

Glioblastoma multiforme (GBM) is the most common and lethal central nervous system tumor. Recently, atovaquone has shown inhibition of signal transducer and activator transcription 3, a promising target for GBM therapy. However, it is currently unable to achieve therapeutic drug concentrations in the brain with the currently reported and marketed formulations. The present study sought to explore the efficacy of atovaquone against GBM as well as develop a formulation of atovaquone that would improve oral bioavailability, resulting in higher amounts of drug delivered to the brain. Atovaquone was formulated as an amorphous solid dispersion using an optimized formulation containing a polymer and a spontaneously emulsifying component (SEC) with greatly improved wetting, disintegration, dispersibility, and dissolution properties. Atovaquone demonstrated cytotoxicity against GBM cell lines as well as provided a confirmed target for atovaquone brain concentrations in in vitro cell viability studies. This new formulation approach was then assessed in a proof-of-concept in vivo exposure study. Based on these results, the enhanced amorphous solid dispersion is promising for providing therapeutically effective brain levels of atovaquone for the treatment of GBM.

show abstract

“…Conversion of crystalline nateglinide into amorphous state also might be another reason for enhancement of solubility. 23…”

Section: Preparation Of Samplementioning

confidence: 99%

Solid Dispersion of Nateglinide in Polyoxy Ethylene-Polyoxy Propylene Block Copolymer: in vitro and in vivo Evaluation

Swain¹,

Subudhi²

2017

IJPER

View full text Add to dashboard Cite

Objective: The study was aimed to improve solubility and bioavailability of nateglinide preparing stable solid dispersions with polyoxy ethylene-polyoxy propylene block copolymer (poloxamer 188). Methods: The solid dispersions were prepared by the melting and solvent technique at 1:1, 1:2, 1:3 (w/w) of drug to carrier ratios. The formulations were characterized by fourier transform infrared spectroscopy, diffrential scanning calorimetry, X-ray diffraction, scanning electron microscopy, dissolution behaviour, stability and in vivo performance. Result and Discussion: The results showed an increase in solubility (52.57 fold) and an enhancement in dissolution of solid dispersions compared to pure nateglinide (P<0.05). FTIR showed retainment of individual peaks indicated few characteristics groups in the drug structure. The DSC thermograms and XRD pattern showed the significant change in crystallinity to amorphous of nateglinide. Pharmacokinetic study was performed in rabbits, showed improved bioavailability (1.71 fold, AUC) of nateglinide in solid dispersions (1:3 w/w). Similarly C max and T max of solid dispersions showed significant difference over the pure drug. Conclusion: The study indicated poloxamer 188 was suitable carrier and melting technique was suitable method for improvement of dissolution and bioavailability of nateglinide.

show abstract

Improvement of solubility, dissolution and stability profile of artemether solid dispersions and self emulsified solid dispersions by solvent evaporation method

Cited by 14 publications

References 27 publications

Physical stability and release properties of lumefantrine amorphous solid dispersion granules prepared by a simple solvent evaporation approach

Physical stability and release properties of lumefantrine amorphous solid dispersion granules prepared by a simple solvent evaporation approach

A Repurposed Drug for Brain Cancer: Enhanced Atovaquone Amorphous Solid Dispersion by Combining a Spontaneously Emulsifying Component with a Polymer Carrier

Solid Dispersion of Nateglinide in Polyoxy Ethylene-Polyoxy Propylene Block Copolymer: in vitro and in vivo Evaluation

Contact Info

Product

Resources

About