การเตรียมยาต้านวัณโรคผงแห้งและการศึกษาในเซลล์มาโครฟาจก่อนการนำมาใช้รักษาวัณโรคปอด

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Insights into the formulation properties, biocompatibility, and permeability of poorly water-soluble methoxyflavones with PEG400 and propylene glycol

Herein, thermal and non-thermal techniques were used to elucidate the putative physical and chemical interactions between poorly water-soluble Kaempferia methoxyflavones and PEG400/propylene glycol. Additionally, the biocompatibility of methoxyflavone-glycol solutions was evaluated using Caco-2 cells whereas the absorptive transport was investigated by measuring the apparent permeability coefficient (Papp) of the methoxyflavones and transepithelial electrical resistance (TEER) of the Caco-2 cell monolayer. Data from differential scanning calorimetry, Fourier-transform infrared (FTIR), and proton nuclear magnetic resonance (1H-NMR) spectroscopic analysis revealed physicochemical compatibility between the three methoxyflavones and PEG400/propylene glycol. Furthermore, PEG400 and propylene glycol solutions of the methoxyflavones were shown to be compatible with Caco-2 cells at pharmacologically effective concentrations. In vitro transport studies across the Caco-2 cell monolayer revealed high Papp values of 24.07 × 10–6 to 19.63 × 10–6 cm s–1 for PEG400 solutions of the methoxyflavones. The TEER values of the Caco-2 cell monolayers indicated that the increased drug transport was partly due to increased tight junction openings, but without compromising the epithelial barrier integrity. The good pharmaceutical and biocompatibility profiles, as well as improved transport of the methoxyflavones in PEG400 and propylene glycol solutions, are suggestive of the worthiness of this approach for further consideration pertaining to the development of these drugs into oral liquid dosage forms

Development of budesonide suspensions for use in an HFA pressurized metered dose inhaler

ABSTRACT: The aim of this study was to develop budesonide as a suspension-based pressurized-metered dose inhaler (pMDI) using hydrofluoroalkanes (HFAs) propellants (HFA 134a, HFA 227, and HFA mixture) and stabilizing agents (oleic acid and sorbitan trioleate). A factorial design method was applied to investigate the effects of two factors (vapour pressure of the propellant system and concentration of stabilizing agents) on formulation performances. Each factor was studied in three levels. Twenty four designed formulations of budesonide suspension-based pMDI were prepared. The results indicated that the vapour pressure of the propellant system was an important factor that affected the content of the active ingredient (p < 0.05). The formulations containing HFA 134a (high level vapour pressure) gave drug contents above the maximum limit (> 120%), whereas the formulations containing HFA 227 (low level vapour pressure) gave low budesonide contents of approximately 50%. However, when a propellant mixture with intermediate vapour pressure was used, the budesonide contents were close to the acceptable range (80-120%). Consequently, the eight formulations containing the HFA mixture together with different types and concentrations of stabilizing agent were tested for their aerosol properties. The fine particle fraction measured by a twin-stage liquid impinger ranged between 32-38%. The mass median aerodynamic diameters obtained from the Andersen cascade impactor were approximately 3 µm for all formulations. No significant difference was found among those formulations. After 3 months of storage, the aerosol properties did not change, and good physical stability was achieved. The particulate budesonide was able to readily re-disperse in the HFA mixture and a homogeneous suspension could be maintained for up to 20 min

Toxicity of fixed oil and crude extract from sa-dao-thiam, Azadirachta excelsa (Jack) seed kernel to Aedes aegypti (L.)

The larvicidal activity of various concentrations of fixed oil and crude extract from sa-dao-thiam, Azadirachta excelsa(Jack) seed kernel was assayed on an Aedes aegypti (L.) test population under controlled laboratory conditions. Concentrationlevels of responses at 24, 48, 72, and 96 hrs were evaluated. The LC50 values of the fixed oil and the crude extract were403.6 and 518.7 ppm, respectively. One hundred percent mortality in 24 hrs-post treatment was achieved at 2,000 and 4,000ppm for the oil and crude extract, respectively. It suggested that the oil is more toxic to Ae. aegypti larvae than the crudeextract. Further investigation suggested the occurrence of molting inhibition of Ae. aegypti larvae by the fixed oil and crudeextract as indicated by the small number of emerged adults. In addition, histological study suggested that damages on theepithelial cells of the midgut could result from the effects of the oil and crude extract. Hypertrophy and degeneration of theepithelial cells were observed, resulting in a presence of some cytoplasmic material in the alimentary canal. Further studiesshould be taken into account to identify their stability and residual activity of these products under field conditions

Evaluation of the topical spray containing Centella asiatica extract and efficacy on excision wounds in rats

Centella asiatica was extracted by methanol. The assay content of triterpenes in the extract was 0.12 % asiatic acid, 0.54 % madecassic acid, 0.25 % asiaticoside and 1.02 % madecassoside. The extract was complexed with hydroxypropyl--cyclodextrin (HP--CD) and formulated with Eudragit E100, glycerol, PEG 400, copovidone, ethanol and purified water. A clear yellowish solution (F1-F8) was obtained. The formulations had a pH of 5.5–6.0 with viscosity in the range of 20–60 mPa s, surface tension 20.3–24.6 mN m–1 and contact angle less than 20. The amount of PEG 400 and copovidone affected the film and spreadability. The content of triterpenes in the spray formulation was close to 100 % compared to triterpenes in the extract. The skin irritation study indicated that the formulation was non-irritating in a rat model. An in vivo excision wound healing model showed that wound excision was completely healed after 14 days

Quantitative analysis of povidone-iodine thin films by X-ray photoelectron spectroscopy and their physicochemical properties

In this study, povidone-iodine (PVP-I) has been formulated as a topical spray to produce a thin film for the controlled release of I2. By means of experimental design, 27 formulations containing glycerol, ethanol, PEG 400, copovidone and HFA 134a as a propellant were prepared. The pH values of all formulations were in the range of 6–7. The viscosity was within the range of 11.9–85.9 mPas. The surface tensions were 20.3 to 24.6 mN m–1 and the contact angles were between 19.3 and 38.7. The assays for the iodine contents were within acceptable range (80–120 %). X-ray photoelectron spectroscopy analysis revealed the ionized form of iodine was much higher than the unionized form. The MIC and MBC values of the PVP-I sprays against Staphylococcus aureus, S. epidermidis and Pseudomonas aeruginosa were higher than that of commercial PVP-I solution. The cytotoxicity study confirmed that the PVP-I spray had lower toxic effects on keratinocytes and fibroblasts compared to the commercial PVP-I solution. The formulation containing 59 % ethanol, 18 % copovidone and 12 % PEG 400 showed good antibacterial activity

The Effect of Sericin from Various Extraction Methods on Cell Viability and Collagen Production

Silk sericin (SS) can accelerate cell proliferation and attachment; however, SS can be extracted by various methods, which result in SS exhibiting different physical and biological properties. We found that SS produced from various extraction methods has different molecular weights, zeta potential, particle size and amino acid content. The MTT assay indicated that SS from all extraction methods had no toxicity to mouse fibroblast cells at concentrations up to 40 μg/mL after 24 h incubation, but SS obtained from some extraction methods can be toxic at higher concentrations. Heat-degraded SS was the least toxic to cells and activated the highest collagen production, while urea-extracted SS showed the lowest cell viability and collagen production. SS from urea extraction was severely harmful to cells at concentrations higher than 100 μg/mL. SS from all extraction methods could still promote collagen production in a concentration-dependent manner, even at high concentrations that are toxic to cells

Formation of Aggregate-Free Gold Nanoparticles in the Cyclodextrin-Tetrachloroaurate System Follows Finke–Watzky Kinetics

Cyclodextrin-capped gold nanoparticles are promising drug-delivery vehicles, but the technique of their preparation without trace amounts of aggregates is still lacking, and the size-manipulation possibility is very limited. In the present study, gold nanoparticles were synthesized by means of 0.1% (w/w) tetrachloroauric acid reduction with cyclodextrins at room temperature, at cyclodextrin concentrations of 0.001 M, 0.002 M and 0.004 M, and pH values of 11, 11.5 and 12. The synthesized nanoparticles were characterized by dynamic light scattering in both back-scattering and forward-scattering modes, spectrophotometry, X-ray photoelectron spectroscopy, transmission electron microscopy and Fourier-transform infrared spectroscopy. These techniques revealed 14.9% Au1+ on their surfaces. The Finke–Watzky kinetics of the reaction was demonstrated, but the actual growth mechanism turned out to be multistage. The synthesis kinetics and the resulting particle-size distribution were pH-dependent. The reaction and centrifugation conditions for the recovery of aggregate-free nanoparticles with different size distributions were determined. The absorbances of the best preparations were 7.6 for α-cyclodextrin, 8.9 for β-cyclodextrin and 7.5 for γ-cyclodextrin. Particle-size distribution by intensity was indicative of the complete absence of aggregates. The resulting preparations were ready to use without the need for concentration, filtration, or further purification. The synthesis meets the requirements of green chemistry

วิธีการใหม่ของการนำส่งยา Propranolol ผ่านทางผิวหนังโดยการใช้ระบบควบคุมการปลดปล่อยที่เลือกเฉพาะอิแนนทิโอเมอร์ : รายงานฉบับสมบูรณ์

Prince of Songkla Universit