Multicomponent systems with cyclodextrins and hydrophilic polymers for the delivery of Efavirenz

Abstract

Efavirenz (EFZ) is one of the most used drugs in the treatment of AIDS and is the first antiretroviral choice. However, since it has low solubility, it does not exhibit suitable bioavailability, which interferes with its therapeutic action and is classified as a class II drug according Biopharmaceutical Classification System (low solubility and high permeability). Among several drug delivery systems, the multicomponent systems with cyclodextrins and hydrophilic polymers are a promising alternative for increasing the aqueous solubility of the drug. The present study aimed to develop and characterize in a ternary system of EFZ, MβCD and PVP K30. The results showed that the solid ternary system provided a large increase in the dissolution rate which was greater than 80% and was characterized by DSC, TG, XRD, FT-IR and SEM. The use of the ternary system (EFZ, MβCD and PVP K30 1%) proved to be a viable, effective and safe delivery of the drug. The addition of the hydrophilic polymer appeared to be suitable for the development of a solid oral pharmaceutical product, with possible industrial scale-up and with low concentration of CDs (cyclodextrins).

Synthesis of Chitosan-Graft- HPβCD Copolymer by Novel One Pot Technique and its application for Solubility Enhancement of Efavirenz

“…Solubility of EFV with grafted copolymer having 1:4 ratio of CS and HPβCD was found to increase solubility of EFV 380 times than that of the free drug. This increase in solubility is higher than the techniques reported earlier such as nanosuspension, 20 solid ternary system containing EFV, MβCD and PVP K30, 21 dendrimerization, 22 composite hydrogel containing HEC-PAA 23 and nanocrystalization. 24 It was observed that with the increase in ratio of HPβCD in graft copolymer (1:1, 1:2, 1:3, 1:4) solubility of EFV was also increased.…”

Hydroxypropyl-β-cyclodextrin as an effective carrier of curcumin – piperine nutraceutical system with improved enzyme inhibition properties

“…Similar approaches have already been reported for different ternary systems, where solubility, stability and potency were modified. For example Vieira, A. C. et al 33 described an increase of solubility and stability for efavirenz according to ternary system formation containing methyl-b-cyclodextrin and polyvinylpyrrolidone K-30. Wang, D. et al 34 noted the enlargement of the solubility and stability of dihydroartemisinin after preparing the ternary system with hydroxypropyl-b-cyclodextrin and lecithin.…”

Formulation and In- Vitro Evaluation of Spherical Crystal Agglomerates of Ebastine by Quasi Emulsion Solvent Diffusion Method

“…This increase was mainly related to spherical shape of SCAs and by increasing in wettability due to the presence of different polymers. PEG 4000 show highest increase in rate of dissolution (f2=20.014) in comparison with pure drug dissolution rate that's because PEG 4000 have important effect on maintaining the spherical shape of agglomerated crystal (36) and also it enhances the physical and chemical stability of drugs and prevents aggregation of the drug particles as a result of the steric hindrance and/or masking of charges provided through formation of a conformational cloud (37) so, higher surface area will be available for dissolution. β.cyclodextrin and TPGS increase in dissolution of EBS (f2= 24.07294) and (f2= 39.46175) respectively due to improvement in solubility.…”

“…On other hand, FTIR spectrum of PEG 4000 show broad band at 3450.99 cm -1 due to O-H group stretching, intense peak at 2885.95 cm -1 due to C-H stretching in addition to an intense band at 1105.98 cm -1 of C-O group (43,44) . FTIR spectrum of the physical mixture of drug and polymers, spherical agglomerated SCAs (EBS1, EBS 6) show no significant shift or reduction in intensity of peaks of EBS, and of β. cyclodextrin, which indicate there was no interaction between drug and polymer.…”