Enhancement of ketoconazole dissolution rate by the liquisolid technique

Molaei, Mir-Ali; Osouli-Bostanabad, Karim; Adibkia, Khosro; Shokri, Javad; Asnaashari, Solmaz; Javadzadeh, Yousef

doi:10.2478/acph-2018-0025

Cited by 25 publications

(19 citation statements)

References 31 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…PVP is used as a solubilizer to enhance the solubility, dissolution rate, and hence bioavailability of poorly soluble drugs in different formulations. The role of PVP in increasing the physical stability of amorphous drugs by preventing the crystallization in the solid-state and maintaining the drug supersaturation after dissolution has been proved in many studies [ 76 , 77 ]. PVP forms water-soluble complexes, because of its hydrophilic nature, with many drugs of low molecular weight, and also avoids crystallization of dissolved drugs.…”

Section: Pharmaceutical and Other Applicationsmentioning

confidence: 99%

“…Molaei et al has conducted a study to improve the dissolution rate of poorly water-soluble drug, ketoconazole by preparing liquid-solid compacts. They used microcrystalline cellulose as a carrier, colloidal silica as a coating material, PEG400 as a nonvolatile solvent and PVP as additive [ 77 ]. In another work, the presence of PVP as an additive in liquid-solid compacts has shown an increased dissolution rate of carbamazepine than the compacts prepared by direct compression [ 76 ].…”

Section: Pharmaceutical and Other Applicationsmentioning

confidence: 99%

See 1 more Smart Citation

Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition

Kurakula

Rao

2020

Journal of Drug Delivery Science and Technology

260

172

View full text Add to dashboard Cite

Polyvinylpyrrolidone (PVP) is a water-soluble polymer obtained by polymerization of monomer N -vinylpyrrolidone. PVP is an inert, non-toxic, temperature-resistant, pH-stable, biocompatible, biodegradable polymer that helps to encapsulate and cater both hydrophilic and lipophilic drugs. These advantages enable PVP a versatile excipient in the formulation development of broad conventional to novel controlled delivery systems. PVP has tunable properties and can be used as a brace component for gene delivery, orthopedic implants, and tissue engineering applications. Based on different molecular weights and modified forms, PVP can lead to exceptional beneficial features with varying chemical properties. Graft copolymerization and other techniques assist PVP to conjugate with poorly soluble drugs that can inflate bioavailability and even introduces the desired swelling tract for their control or sustained release. The present review provides chemistry, mechanical, physicochemical properties, evaluation parameters, dewy preparation methods of PVP derivatives intended for designing conventional to controlled systems for drug, gene, and cosmetic delivery. The past and growing interest in PVP establishes it as a promising polymer to enhance the trait and performance of current generation pharmaceutical dosage forms. Furthermore, the scrutiny explores existing patents, marketed products, new and futuristic approaches of PVP that have been identified and scope for future development, characterization, and its use. The exploration spotlights the importance and role of PVP in the design of Povidone-iodine (PVP–I) and clinical trials to assess therapeutic efficacy against the COVID-19 in the current pandemic scenario.

show abstract

Section: Pharmaceutical and Other Applicationsmentioning

confidence: 99%

Section: Pharmaceutical and Other Applicationsmentioning

confidence: 99%

Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition

Kurakula

Rao

2020

Journal of Drug Delivery Science and Technology

260

172

View full text Add to dashboard Cite

show abstract

“…Its very low solubility in water, 0.017 mg/mL, makes its formulation challenging because of the incomplete dissolution that causes low and variable bioavailability. In the last years, there was an increasing interest in the formulation approaches for solubility enhancement of KET, including complexes with β-cyclodextrins, hot-melt extrusion, nanosuspensions, , solid dispersion, coamorphous, , and liquisolid systems . Another important way to enhance the solubility, dissolution rate, and bioavailability of active pharmaceutical ingredients is crystal engineering by salt/cocrystal formation .…”

Section: Introductionmentioning

confidence: 99%

Ketoconazole-p-aminobenzoic Acid Cocrystal: Revival of an Old Drug by Crystal Engineering

Martin

Pop²,

Kacsó

et al. 2020

Mol. Pharmaceutics

View full text Add to dashboard Cite

The 1:1 cocrystal of the antifungal agent ketoconazole with p-aminobenzoic acid was successfully crystallized and systematically characterized by a physical and pharmacological point of view. Crystal structure determination confirmed the cocrystal identity, giving full insight in its crystal packing and degree of disorder. Powder dissolution measurements revealed a 10-fold aqueous solubility increase that induces a 6.7-fold oral bioavailability improvement compared to ketoconazole. In vitro cell assays showed a good toxicity profile of the cocrystal with lower oxidative stress and inflammation and enhanced antifungal activity against several Candida species. The in vivo study of the cocrystal indicated similar pharmacokinetic profiles and liver toxicity with increased transaminases, as reported for ketoconazole. Notably, besides minor signs of inflammation, no morphological changes in liver parenchyma or signs of fibrosis and necrosis were detected. The enhanced solubility and oral bioavailability of the cocrystal over ketoconazole, together with the improved antifungal activity and good in vitro/in vivo toxicity, indicate its potential use as an alternative antifungal agent to the parent drug. Our results bring evidence of cocrystallization as a successful approach for bioavailability improvement of poorly soluble drugs.

show abstract

“…For class II drugs based on Biopharmaceutical Classification System (BCS) (with limited water solubility and high permeability), the dissolution rate in the GIT usually controls the oral absorption rate. 12 Therefore, along with permeability, a drug dissolution rate and/or solubility are key factors that determine its oral bioavailability. 13 This evidence proposes that the enhanced GIT absorption of GLC could be acquired using its augmented release formulations which increase the dissolution rate and consequently improve bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

et al. 2019

Self Cite

View full text Add to dashboard Cite

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

show abstract

Enhancement of ketoconazole dissolution rate by the liquisolid technique

Cited by 25 publications

References 31 publications

Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition

Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition

Ketoconazole-p-aminobenzoic Acid Cocrystal: Revival of an Old Drug by Crystal Engineering

Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

Contact Info

Product

Resources

About