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. 2021 Aug 23;13(8):1315.
doi: 10.3390/pharmaceutics13081315.

VSports最新版本 - Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

Nayyer Islam  1 , Muhammad Irfan  1 , Ameer Fawad Zahoor  2 , Muhammad Shahid Iqbal  3 , Haroon Khalid Syed  1 , Ikram Ullah Khan  1 , Akhtar Rasul  1 , Salah-Ud-Din Khan  4 , Alaa M Alqahtani  5 , Muzzamil Ikram  6 , Muhammad Abdul Qayyum  7 , Ahmed Khames  8 , Sana Inam  1 , Mohammed A S Abourehab  9   10
Affiliations

"VSports" Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

"V体育ios版" Nayyer Islam et al. Pharmaceutics. .

Abstract

The main objective of this research work was the development and evaluation of transfersomes integrated oral films for the bioavailability enhancement of Ebastine (EBT) to treat allergic rhinitis. The flexible transfersomes, consisting of drug (EBT), lipid (Phosphatidylcholine) and edge activator (EA) Polyoxyethylene sorbitan monooleate or Sorbitan monolaurate, were prepared with the conventional thin film hydration method. The developed transfersomes were further integrated into oral films using the solvent casting method. Transfersomes were evaluated for their size distribution, surface charge, entrapment efficiency (EE%) and relative deformability, whereas the formulated oral films were characterized for weight, thickness, pH, folding endurance, tensile strength, % of elongation, degree of crystallinity, water content, content uniformity, in vitro drug release and ex vivo permeation, as well as in vivo pharmacokinetic and pharmacodynamics profile. The mean hydrodynamic diameter of transfersomes was detected to be 75. 87 ± 0. 55 nm with an average PDI and zeta potential of 0. 089 ± 0. 01 and 33. 5 ± 0. 39 mV, respectively. The highest deformability of transfersomes of 18. 52 mg/s was observed in the VS-3 formulation. The average entrapment efficiency of the transfersomes was about 95. 15 ± 1. 4%. Transfersomal oral films were found smooth with an average weight, thickness and tensile strength of 174. 72 ± 2. 3 mg, 0. 313 ± 0. 03 mm and 36. 4 ± 1. 1 MPa, respectively. The folding endurance, pH and elongation were found 132 ± 1, 6. 8 ± 0. 2 and 10 VSports手机版. 03 ± 0. 4%, respectively. The ex vivo permeability of EBT from formulation ETF-5 was found to be approximately 2. 86 folds higher than the pure drug and 1. 81 folds higher than plain film (i. e. , without loaded transfersomes). The relative oral bioavailability of ETF-5 was 2. 95- and 1. 7-fold higher than that of EBT-suspension and plain film, respectively. In addition, ETF-5 suppressed the wheal and flare completely within 24 h. Based on the physicochemical considerations, as well as in vitro and in vivo characterizations, it is concluded that the highly flexible transfersomal oral films (TOFs) effectively improved the bioavailability and antihistamine activity of EBT. .

Keywords: bioavailability; ebastine; edge activator; in vivo; phospholipids; transfersomes. V体育安卓版.

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Conflict of interest statement (VSports最新版本)

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Schematic representation of the transfersomes formulation process.
Figure 2
Figure 2
Transfersomes (A) size and charge, (B) entrapment efficiency and deformability.
Figure 3
Figure 3
FTIR spectra of (A) EBT, (B) PC, (C) Tween 80®, (D) Span 20® and (E) optimized formulation ETF-5.
Figure 4
Figure 4
Scanning electron microscopy photographs of (A) EBT and (B) ETF-5 film.
Figure 5
Figure 5
Illustration of surface morphology of optimized formulation (ETF-5) of transfersomes-loaded oral films (TOFs).
Figure 6
Figure 6
Powder X-ray diffraction of (A) EBT and optimized formulation (B) ETF-5.
Figure 7
Figure 7
DSC thermograms of (A) EBT and (B) oral film loaded with optimized transfersomes (ETF-5-TOFs).
Figure 8
Figure 8
Cumulative in vitro drug release (%) from EBT suspension, EBT plain film and optimized formulation ETF-5.
Figure 9
Figure 9
Ex vivo permeation studies of EBT suspension, EBT plain film and ETF-5 formulation.
Figure 10
Figure 10
Mean plasma concentration-time profile for carebastine following oral treatment of EBT suspension, EBT plain film and ETF5.
See this image and copyright information in PMC

References (VSports在线直播)

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