Ruchadaporn Kaomongkolgit

Fabrication of a novel scaffold of clotrimazole-microemulsion-containing nanofibers using an electrospinning process for oral candidiasis applications.

Clotrimazole (CZ)-loaded microemulsion-containing nanofiber mats were developed as an alternative for oral candidiasis applications. The microemulsion was composed of oleic acid (O), Tween 80 (T80), and a co-surfactant such as benzyl alcohol (BzOH), ethyl alcohol (EtOH) or isopropyl alcohol (IPA). The nanofiber mats were obtained by electrospinning a blended solution of a CZ-loaded microemulsion and a mixed polymer solution of 2% (w/v) chitosan (CS) and 10% (w/v) polyvinyl alcohol (PVA) at a weight ratio of 30:70. The nanofiber mats were characterized using various analytical techniques. The entrapment efficiency, drug release, antifungal activity and cytotoxicity were investigated. The average diameter of the nanofiber mats was in the range of 105.91-125.56 nm. The differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD) results revealed the amorphous state of the CZ-loaded microemulsions incorporated into the nanofiber mats. The entrapment efficiency of CZ in the mats was approximately 72.58-98.10%, depended on the microemulsion formulation. The release experiment demonstrated different CZ release characteristics from nanofiber mats prepared using different CZ-loaded microemulsions. The extent of drug release from the fiber mats at 4h was approximately 64.81-74.15%. The release kinetics appeared to follow Higuchis model. In comparison with CZ lozenges (10mg), the nanofiber mats exhibited more rapid killing activity. Moreover, the nanofiber mats demonstrated desirable mucoadhesive properties and were safe for 2h. Therefore, the nanofiber mats have the potential to be promising candidates for oral candidiasis applications.

Fast releasing oral electrospun PVP/CD nanofiber mats of taste-masked meloxicam

Fast release and taste masking of meloxicam (MX)-loaded polyvinylpyrrolidone (PVP)/cyclodextrin (CD) nanofiber mats were developed using an electrospinning process. CDs were blended to improve the stability of the mats. The morphology and diameter of the mats were determined using scanning electron microscopy (SEM); physical and mechanical properties were also studied. The MX content, disintegration time, MX release and cytotoxicity of the mats were investigated. In vivo studies were also performed in healthy human volunteers. The results indicated that the mats were successfully prepared with fiber in the nanometer range. MX was well incorporated into the mats, with an amorphous form. The mats showed suitable tensile strength. CDs improved the physical stability by their cage-like supramolecular structure to protect from humidity and moisture, and create bead free nanofiber mats. The nanofiber mats with CDs were physically stable without any hygroscopicity and fusion. A fast disintegration and release of MX was achieved. Moreover, this mat released MX faster than the MX powder and commercial tablets. The cytotoxicity test revealed that mats were safe for a 5-min incubation. The disintegration studies indicated that in vivo disintegration agreed with the in vitro studies; the mat rapidly disintegrated in the mouth. The less bitter of MX was occurred in the mats that incorporated CD, menthol and aspartame. In addition, this mat was physical stable for 6 months. The results suggest that these mats may be a good candidate for fast dissolving drug delivery systems of bitter drugs to increase the palatability of dosage forms.

Apoptotic effect of alpha-mangostin on head and neck squamous carcinoma cells.

OBJECTIVE The purposes of this study were to measure the cytotoxic effect of alpha-mangostin on head and neck squamous cell carcinoma (HNSCC) cell lines, to evaluate the apoptotic aspect of dead cells, and to identify the molecular mechanism involved in apoptosis. METHODS The human HNSCC cell lines HN-22, HN-30 and HN-31 were treated with alpha-mangostin. The apoptotic effects of alpha-mangostin on HNSCC cells were determined by observation the morphological changes of cells, immunofluorescence for single-stranded DNA (ssDNA), and DNA fragmentation analysis. The expression of bax, bcl-2, and p53 were detected by RT-PCR and Western blot analysis. RESULTS Alpha-mangostin showed excellent apoptotic effects on HNSCC cell lines, which induced the down-regulation of bcl-2, but up-regulation of bax and p53 in HN-22, HN-30 and HN-31. CONCLUSION The present study suggests that the induction of apoptosis by alpha-mangostin seemed to be modulated by bcl-2, bax and p53 level in HNSCC cell lines.

Mucoadhesive electrospun chitosan-based nanofibre mats for dental caries prevention

The mucoadhesive electrospun nanofibre mats were developed using chitosan (CS) and thiolated chitosan (CS-SH) as mucoadhesive polymers. Garcinia mangostana (GM) extract was incorporated into nanofibre mats. The antibacterial activity in the single and combined agents was evaluated against dental caries pathogens. The morphology of mats was observed using SEM. The mats were evaluated for GM extract amount, mucoadhesion, in vitro release, antibacterial activity and cytotoxicity. The mucoadhesion and antibacterial activity were determined in healthy human volunteers. The prepared mats were in nanoscale with good physical and mucoadhesive properties. The CS-SH caused the higher mucoadhesion. All mats rapidly released active substances, which had the synergistic antibacterial activity. In addition, the reduction of bacteria and good mucoadhesion in the oral cavity occurred without cytotoxicity. The results suggest that mats have the potential to be mucoadhesive dosage forms to maintain oral hygiene by reducing the bacterial growth that causes the dental caries.

Fabrication of mucoadhesive chitosan coated polyvinylpyrrolidone/cyclodextrin/clotrimazole sandwich patches for oral candidiasis

This study aims to fabricate clotrimazole (CZ)-composite sandwich nanofibers using electrospinning. The CZ-loaded polyvinylpyrrolidone (PVP)/hydroxypropyl-β-cyclodextrin (HPβCD) fiber was coated with chitosan-cysteine (CS-SH)/polyvinyl alcohol (PVA) to increase the mucoadhesive properties and to achieve a sustained release of the drug from the nanofibers. The nanofibers were characterized using scanning electron microscopy (SEM), Fourier transform infrared (FT-IR) spectroscopy and X-ray diffractometry (XRD). The nanofibers mechanical and mucoadhesive properties, drug release, antifungal activity and cytotoxicity were also assessed. The fibers were in the nanoscale with good mucoadhesive properties. The XRPD revealed a molecular dispersion of amorphous CZ in the nanofibers. The initial fast release of CZ from the nanofibers was achieved. Moreover, the sandwich nanofibers coated for longer times resulted in slower release rates compared with the shorter coating times. The CZ-loaded nanofibers killed the Candida significantly faster than the commercial CZ lozenges at 5, 15 and 30 min and were safe for a 2-h incubation. Therefore, these nanofibers may be promising candidates for the treatment of oral candidiasis.

Fast-Acting Clotrimazole Composited PVP/HPβCD Nanofibers for Oral Candidiasis Application

ABSTRACTPurposeThis study investigates fabrication of clotrimazole (CZ)-composited electrospun Polyvinylpyrrolidone/Hydroxypropyl-β-cyclodextrin (PVP/HPβCD) blended nanofiber mats for oral candidiasis applications.MethodsPVP/HPβCD blended nanofiber mats containing clotrimazole were electrospun and characterized using SEM, DSC and XRPD. The solvent system ethanol: water: benzyl alcohol (EtOH:H2O:BzOH) with a 70:20:10 ratio was optimal for the electrospinning process. Various amounts of CZ were loaded into the nanofiber mats. The nanofiber mats was further investigated for drug release, antifungal activity and cytotoxicity.ResultsThe fiber diameters in the mats were in the nanometer range. The DSC and XRPD revealed a molecular dispersion of amorphous CZ in the nanofiber mats. The loading capacity increased when CZ content was raised. A fast dissolved and released of CZ from the nanofibers mat was achieved. The ability of the CZ-loaded nanofiber mats to kill the Candida depended on the amount of CZ in the mats; moreover, the CZ-loaded nanofibers killed the Candida significantly faster than the CZ powder and lozenges with low cytotoxicity.ConclusionsCZ-loaded nanofiber mats were successfully electrospun. They exhibited rapid antifungal activity in vitro relative to CZ powder and lozenges. Further in vivo studies are needed to investigate for their application in oral candidiasis.

Alpha-mangostin suppresses MMP-2 and MMP-9 expression in head and neck squamous carcinoma cells.

The purpose of this study was to investigate the effect of alpha-mangostin on matrix metalloproteinase (MMP)-2 and MMP-9 expression in head and neck squamous cell carcinoma (HNSCC). The human HNSCC cell lines were treated with alpha-mangostin and the cytotoxicity of alpha-mangostin in HNSCC was determined using the MTS assay. To determine the effect of alpha-mangostin on the expression of MMP-2 and MMP-9 in HNSCC, gelatin zymography and RT-PCR were performed. The results showed that alpha-mangostin increased in growth inhibition of HNSCC cell lines in a concentration-dependent manner. Treatment with alpha-mangostin decreased MMP-2 and MMP-9 expression in a concentration-dependent manner in all cell lines. These findings suggested that alpha-mangostin might be a potential therapeutic agent for HNSCC.

Antifungal activity of coronarin D against Candida albicans.

OBJECTIVE The objective of this study was to investigate the antifungal activity of coronarin D on Candida albicans and its activity was compared with clotrimazole and nystatin. METHODS Coronarin D was extracted by liquid chromatography and used in antifungal testing. The inhibitory effect of coronarin D on C. albicans was determined by cultures and an applied broth dilution test. The rate of fungicidal activity was evaluated by time-kill curves. Morphologic alterations of fungal cells were investigated using scanning electron microscopy. RESULTS Coronarin D was effective against C. albicans; the minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) were 2 and 4 mg/mL, respectively. The C. albicans killing activity of coronarin D was higher than clotrimazole and nystatin at 2 × MFC and 4 × MFC, respectively. Morphologic alterations of fungal cells consistent with cell membrane damage were observed in the coronarin D-treated cells. CONCLUSIONS Coronarin D showed promising antifungal activity against C. albicans in vitro.

Fabrication and Evaluation of Nanostructured Herbal Oil/Hydroxypropyl-β-Cyclodextrin/Polyvinylpyrrolidone Mats for Denture Stomatitis Prevention and Treatment

This work aims to develop the herbal oil-incorporated nanostructure mats with antifungal activity for the prevention and treatment of Candida-associated denture stomatitis. The nanofiber mats loaded with betel oil or clove oil were fabricated via electrospinning process. The morphologies and physicochemical properties of the herbal oil loaded nanofiber mats were examined using scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and mechanical testing. The release characteristic, antifungal activity, and cytotoxicity were also investigated. The SEM images confirmed the homogeneous and smooth nanoscale fibers. The addition of the herbal oil into the nanofiber mats reduced the fiber diameters. The DSC and FT-IR results confirmed the presence of the oil in the nanofiber mats. The herbal oils can be released from the mats in a very fast manner and inhibit the growth of candida cells within only few minutes after contact. These nanofiber mats may be beneficial for the prevention and treatment of denture stomatitis.

Pyoderma gangrenosum-like oral ulcerations in an elderly patient

OBJECTIVE To present a case of pyoderma gangrenosum (PG)-like oral ulcerations in an elderly patient. BACKGROUND PG is an uncommon idiopathic, ulcerative, chronic inflammatory cutaneous disorder of unknown etiology, which is associated with systemic diseases found in more than 50% of patients. Oral lesions of PG are extremely rare and have not been previously reported on chronic leukemia patient. CLINICAL REPORT This report presents the first case of a 73 year-old man who had PG-like oral ulcerations which offered the possibility of an initial finding of chronic myeloid leukemia. CONCLUSION Clinicians should always take into consideration that PG in the oral mucosa is a recalcitrant ulcer and can precede the development of underlying clonal malignancy.