ArticleAAPS PharmSciTech2009
Physicochemical characterization of efavirenz-cyclodextrin inclusion complexes.
Article in AAPS PharmSciTech, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed.
- A case study on decentralized manufacturing of 3D printed medicines.International journal of pharmaceutics: X · 2023Article
- The Impact of Process and Formulation Parameters on the Fabrication of Efavirenz Nanosuspension to Improve Drug Solubility and Dissolution.Iranian journal of pharmaceutical research : IJPR · 2022Article
- Formulation and characterization of eprosartan mesylate and β-cyclodextrin inclusion complex prepared by microwave technology.Drug delivery · 2022Article
- Hispolon Cyclodextrin Complexes and Their Inclusion in Liposomes for Enhanced Delivery in Melanoma Cell Lines.International journal of molecular sciences · 2022Article
- Identification of a βCD-Based Hyper-Branched Negatively Charged Polymer as HSV-2 and RSV Inhibitor.International journal of molecular sciences · 2022Article
- Amorphous Inclusion Complexes: Molecular Interactions of Hesperidin and Hesperetin with HP-Β-CD and Their Biological Effects.International journal of molecular sciences · 2022Article
- Nanotechnology-based antiviral therapeutics.Drug delivery and translational research · 2021Review
- Review
- Cyclodextrins in Antiviral Therapeutics and Vaccines.Pharmaceutics · 2021Review
- Inclusion Compound of Efavirenz and γ-Cyclodextrin: Solid State Studies and Effect on Solubility.Molecules (Basel, Switzerland) · 2021Article
- Formulation and optimization of liquisolid compact for enhancing dissolution properties of efavirenz by using DoE approach.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2020Article
- Kinetic estimation of solid state transition during isothermal and grinding processes among efavirenz polymorphs.Heliyon · 2020Article
- Enhanced pharmacological efficacy of sumatriptan due to modification of its physicochemical properties by inclusion in selected cyclodextrins.Scientific reports · 2018Article
- Nano-ART and NeuroAIDS.Drug delivery and translational research · 2016Review
- Getting into the brain: Potential of nanotechnology in the management of NeuroAIDS.Advanced drug delivery reviews · 2016Review
- The Role of Nanoparticle in Brain Permeability: An in-vitro BBB Model.Iranian journal of pharmaceutical research : IJPR · 2016Article
- A Self-microemulsifying Drug Delivery System (SMEDDS) for a Novel Medicative Compound Against Depression: a Preparation and Bioavailability Study in Rats.AAPS PharmSciTech · 2015Article
- Effects of the Preparation Method on the Formation of True Nimodipine SBE-β-CD/HP-β-CD Inclusion Complexes and Their Dissolution Rates Enhancement.AAPS PharmSciTech · 2015Article
- SN-38-cyclodextrin complexation and its influence on the solubility, stability, and in vitro anticancer activity against ovarian cancer.AAPS PharmSciTech · 2014Article
- Formulation and evaluation of fixed-dose combination of bilayer gastroretentive matrix tablet containing atorvastatin as fast-release and atenolol as sustained-release.BioMed research international · 2014Article
Corrections and comments
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Efavirenz (EFV) is an oral antihuman immunodeficiency virus type 1 drug with extremely poor aqueous solubility. Thus, its gastrointestinal absorption is limited by the dissolution rate of the drug. The objective of this study was to characterize the inclusion complexes of EFV with beta-cyclodextrin (beta-CD), hydroxypropyl beta-CD (HPbetaCD), and randomly methylated beta-CD (RMbetaCD) to improve the solubility and dissolution of EFV. The inclusion complexation of EFV with cyclodextrins in the liquid state was characterized by phase solubility studies. The solid-state characterization of various EFV and CD systems was performed by X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy analyses. Dissolution studies were carried out in distilled water using US Pharmacopeia dissolution rate testing equipment. Phase solubility studies provided an A(L)-type solubility diagram for beta-CD and A(P)-type solubility diagram for HPbetaCD and RMbetaCD. The phase solubility data enabled calculating stability constants (K (s)) for EFV-betaCD, EFV-HPbetaCD, and EFV-RMbetaCD systems which were 288, 469, and 1,073 M(-1), respectively. The physical and kneaded mixtures of EFV with CDs generally provided higher dissolution of EFV as expected. The dissolution of EFV was substantially higher with HPbetaCD and RMbetaCD inclusion complexes prepared by the freeze drying method. Thus, complexation with HPbetaCD and RMbetaCD could possibly improve the dissolution rate-limited absorption of EFV.
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