Abstract
The work herein presented aims to develop and characterize carvedilol (CVD) releasable non-water-soluble monolayers and a multilayer patch made of ultrathin micron and submicron fibers for drug delivery into the sublingual mucosa. Firstly, the developed formulations containing CVD within different biopolymers (PDLA, PCL, and PHB) were characterized by scanning electron microscopy (SEM), attenuated total reflectance Fourier transformed infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC), wide-angle X-ray scattering (WAXS), and for their in vitro drug release. SEM micrographs assessed the fiber morphology attained by adding carvedilol. ATR-FTIR spectra revealed good chemical compatibility between CVD and the tested biopolymers, whereas DSC and WAXS confirmed that CVD was in an amorphous state within the biopolymeric fibers. In vitro release studies showed enhanced CVD release kinetics from the electrospun biopolymer monolayers compared to the dissolution rate of the commercial form of the pure drug, except for the slow-releasing PDLA fibers. Finally, the selected CVD-loaded layer, i.e., electrospun PHB, was built into a three-layer patch to tackle mucosa adhesion and unidirectional release, while retaining the enhanced release kinetics. The patch design proposed here further demonstrates the potential of the electro-hydrodynamic processing technology to render unique mucoadhesive controlled delivery platforms for poorly water-soluble drugs.
Highlights
A large proportion of new drug candidates present poor water solubility, whilst others present a strong first-pass effect, limiting their use in potential medical therapies [1,2].In light of this, researchers are focusing their efforts on searching for novel technologies and formulations that can aid to improve the bioavailability and solubility of these active pharmaceutical ingredients (APIs) [3,4,5]
It is well known that the physicochemical properties of polymer solutions play an important role in electrospinning processability and in the final fiber morphology of the material [30,31]
The results indicated that the CVD loading in the fibers was 9.41 ± 0.32% for PCL-CVD-loaded fibers, 10.45 ± 0.39% for PHB fibers, and 10.11 ± 0.54% for PDLA fibers
Summary
A large proportion of new drug candidates present poor water solubility, whilst others present a strong first-pass effect, limiting their use in potential medical therapies [1,2].In light of this, researchers are focusing their efforts on searching for novel technologies and formulations that can aid to improve the bioavailability and solubility of these active pharmaceutical ingredients (APIs) [3,4,5]. Interest has been focused on the generation of mucoadhesive delivery platforms to enhance drug permeability and solubility. In this sense, sublingual mucoadhesive systems for API release can become a competitive alternative to traditional delivery systems [6]. Sublingual mucoadhesive systems for API release can become a competitive alternative to traditional delivery systems [6] This route goes directly to the systemic circulation through the internal jugular vein [7], avoiding drug degradation in the gastrointestinal tract or its metabolization via the first-pass effect [6,8]. The sublingual mucosa can promote a rapid pharmacological onset, whilst providing a simple and non-invasive approach that facilitates drug administration for patients with swallowing difficulties [9]
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