Engineering and Development of Chitosan-Based Nanocoatings for Ocular Contact Lenses.

This article reports on electrohydrodynamic atomization to engineer on-demand novel coatings for ocular contact lenses. A formulation approach was adopted to modulate the release of timolol maleate (TM) using chitosan and borneol. Polymers polyvinylpyrrolidone and poly (N-isopropylacrylamide) were utilized to encapsulate TM and were electrically atomized to produce optimized, stationary contact lens coatings. The particle and fiber diameter, thermal stability, material compatibility of the formed coatings, their in vitro release-modulating effect, and ocular tolerability were investigated. Results demonstrated highly stable nanomatrices with advantageous morphology and size. All formulations yielded coatings with high TM encapsulation (>88%) and excellent ocular biocompatibility. Coatings yielded biphasic and triphasic release, depending on composition. Kinetic modeling revealed a noticeable effect of chitosan; the higher the concentration, the more the release of TM because of chitosan swelling, with the mechanism changing from Fickian diffusion (1% w/v; n = 0.5) to non-Fickian (5% w/v, 0.45

Ex vivo buccal drug delivery of ropinirole hydrochloride in the presence of permeation enhancers: the effect of charge.

In the current study, the ex vivo permeation of ropinirole hydrochloride (RH) across porcine buccal mucosa in the presence of three permeation enhancers, namely N-trimethyl chitosan (TMC) (positively charged) a chitosan derivative, sulfobutyl ether-ß-cyclodextrin (SBE-ß-CD) (negatively charged) and hydroxypropyl-ß-cyclodextrin (HP-ß-CD) (neutral), was investigated. Buccal permeation studies were conducted using Franz diffusion cells. Cumulative amounts of RH were plotted versus time. The presence of the permeation enhancers significantly increased the transport of the drug across the porcine buccal epithelium compared to its plain congener (RH solution). The rank order effect of the permeation enhancers for the transport of RH across buccal epithelium was TMC ≥ SBE-ß-CD > HP-ß-CD > RH solution. The presence of TMC increased 1.34-fold the transport of RH across buccal epithelium, whereas an increase of 1.23- and 1.28-fold was reported in the presence of HP-ß-CD and SBE-ß-CD, respectively. Infrared spectroscopy (IR) was employed to investigate the interaction of permeation enhancers with the epithelial lipids of porcine buccal mucosa corroborating the permeation results. Finally, light microscopy was performed to assess the histological changes in the porcine epithelium. Formation of vacuoles, spongiosis and acantholysis linear detachment and destruction of the epithelium resulted from the presence of the permeation enhancers. The data suggest that all enhancers tested, and particularly TMC, increase the transport of RH across buccal epithelium.

Pharmaceutical and biomaterial engineering via electrohydrodynamic atomization technologies.

Complex micro- and nano-structures enable crucial developments in the healthcare remit (e.g., pharmaceutical and biomaterial sciences). In recent times, several technologies have been developed and explored to address key healthcare challenges (e.g., advanced chemotherapy, biomedical diagnostics and tissue regeneration). Electrohydrodynamic atomization (EHDA) technologies are rapidly emerging as promising candidates to address these issues. The fundamental principle driving EHDA engineering relates to the action of an electric force (field) on flowing conducting medium (formulation) giving rise to a stable Taylor cone. Through careful optimization of process parameters, material properties and selection, nozzle and needle design, and collection substrate method, complex active micro- and nano-structures are engineered. This short review focuses on key selected recent and established advances in the field of pharmaceutical and biomaterial applications.

Preparation and characterization of bioadhesive microparticles comprised of low degree of quaternization trimethylated chitosan for nasal administration: effect of concentration and molecular weight.

Toward the development of microparticulate carriers for nasal administration, N-trimethylchitosan chloride (TMC) of low molecular weight (LMW) and high molecular weight (HMW) and low degree of quaternization (16% and 27%, respectively) was co-formulated into microparticles comprising of dipalmatoylphosphatidylcholine (DPPC) and poly(lactic-co-glycolic) acid (PLGA) via the spray-drying technique. The chitosan derivatives were characterized by means of nuclear magnetic resonance (NMR), differential scanning calorimetry (DSC), and Fourier transfrom infrared (FTIR) spectroscopy. The size and morphology of the produced microparticles were assessed by scanning electron microscopy (SEM), whereas their mucoadhesive properties were investigated by means of atomic force microscopy-force spectroscopy (AFM-FS). The results showed that microparticles exhibit mucoadhesion when TMC is present on their surface above a threshold of TMC (>0.3% w/w).

Preparation and characterization of multiactive electrospun fibers: poly-ɛ-carpolactone fibers loaded with hydroxyapatite and selected NSAIDs.

Electrospun poly-ε-caprolactone fibers were employed as hosts for hydroxypatite and nonsteroidal anti-inflammatory drugs (NSAIDs) ibuprofen (IBU) and indomethacin (INDO) (separately). The fibers (size range between 400 and 20 µm) were characterized by means of X-ray diffraction, differential scanning calorimetry, fourier-transform infrared spectroscopy and scanning electron microscopy. The physicochemical characterization of the fibers indicated that the drugs are associated with the fibers in an amorphous state. The release of IBU and INDO was monitored in PBS pH 7.4. A rapid release was observed for both drugs. Finally, bioactivity studies in simulated body fluid revealed the formation of hydroxyapatite, indicating that the fibers could be further utilized as materials for coupled (or multipurpose) biomedical and biomaterial engineering applications.

Hydrogels in mucosal delivery.

The concept of mucoadhesion and the molecular design requirements for the synthesis of mucoadhesive agents are both well understood and, as a result, hydrogel formulations that may be applied to mucosal surfaces are readily accessible. Nanosized hydrogel systems that make use of biological recognition or targeting motifs, by reacting to disease-specific environmental triggers and/or chemical signals to affect drug release, are now emerging as components of a new generation of therapeutics that promise improved residence time, faster response to stimuli and triggered release.