Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone

Abstract

The aim of this study was to improve the solubility of amiodarone hydrochloride (AMD) and the drug release using its inclusion complexes with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complexes were prepared by coprecipitation and freeze-drying. The solubility enhancement of AMD/HP-β-CD inclusion complexes by 4–22 times was evaluated by the phase solubility method. The inclusion complexes were studied both in solution and in solid state by spectroscopic methods, dynamic light scattering (DLS) and zeta potential analysis, SEM, and DSC. The formulations of AMD/HP-β-CD inclusion complexes both as powdered form and as matrix tablets showed superior pharmacokinetic performance in improving loading and release properties in respect of those of the insoluble AMD drug. In vitro kinetic study reveals a complex mechanism of release occurring in three steps: the first one being attributed to a burst effect and the other two to different bonding existing in inclusion complexes. An in vivo test on matrix tablets containing Kollidon® and chitosan also reveals a multiple (at least two) peaks release diagram because of both structures of the inclusion complexes and also of different sites of absorption in biological media (digestive tract).

Structural Investigation of Hesperetin-7-O-Glucoside Inclusion Complex with β-Cyclodextrin: A Spectroscopic Assessment

“…The results revealed that the zeta potential was lowered when the HEPT7G moiety was included in the β-CD cavity. This can be attributed to the blocking of the –OH group by the HEPT7G moiety inclusion through an electrostatic attraction between the acidic phenolic –OH groups of the HEPT7G moiety and the charge-influenced distribution of β-CD particles [ 85 , 86 ]. Therefore, an enhancement in the surface charge could be attributed to the formation of hydrogen bonding between the β-CD and charged HEPT7G moiety head groups.…”

Investigating the Interaction of Anthracene and Phenanthrene with Cucurbit[n]urils (n=6‐8): Experimental and Molecular Dynamics Studies

“…As a result of the inclusion complexation, several of the guest protons resonance experience significant changes in chemical shift. On interaction, changes in chemical shifts are expected for protons of both host and guest molecules as a result of loss of magnetic field homogeneity and induced conformational restrictions leading to changes in the shape and position of the peaks [41] . Pure PHN exhibits five aromatic protons peaks (assigned according to the structure in Figure 1d) ranging from 8.825 ppm to 7.650 ppm, which are shifted when it interacts with the hosts in DMSO, Figure 6.…”

Polymer Microparticles Prolong Delivery of the 15-PGDH Inhibitor SW033291

“…Molecular structure data files for SW033291 were downloaded from PubChem and cyclodextrin variants (α-CD, β-CD, and γ-CD) were isolated using Jmol v. 14 (http://www.jmol.org/, accessed on 7 October 2021) from Protein Data Bank entries 1CXF, 3CGT, and 1D3C, respectively. Previous studies have shown that "binding affinity", represented by K D , is closely correlated with the duration of drug delivery, and that drug complexation with CD does not impact the chemical properties of the drug payload [11,[18][19][20].…”