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1.
Prasert Akkaramongkolporn Tanasait Ngawhirunpat Praneet Opanasopit 《AAPS PharmSciTech》2009,10(2):641-648
The differently sulfonated styrene–divinylbenzene cross-linked copolymer cationic exchange resins were prepared by oil-in-water
polymerization and varied degrees of sulfonation. Several characteristics of the obtained resins were evaluated, i.e., Fourier
transform infrared spectra, the ion-exchange capacity, microscopic morphology, size, and swelling. The resin characteristics
were altered in relation to the degree of sulfonation, proving that differently sulfonated resins could be prepared. The behavior
of chlorpheniramine (CPM) loading and in vitro release in the USP simulated gastric (SGF) and intestinal fluids (SIF) of the obtained resins were also evaluated. The CPM
loaded in the resinates (drug-loaded resins) increased with the increasing degree of sulfonic group and hence the drug binding
site in the employed resins. The CPM release was lower from the resins with the higher degree of sulfonic group due to the
increase in the diffusive path depth. The CPM release was obviously lower in SGF than SIF because CPM, a weak base drug, ionized
to a greater extent in SGF and then preferred binding with rather than releasing from the resins. In conclusion, the differently
sulfonated resins could be utilized as novel carriers for drug delivery. 相似文献
2.
Wipada Samprasit Prasert Akkaramongkolporn Tanasait Ngawhirunpat Theerasak Rojanarata Praneet Opanasopit 《AAPS PharmSciTech》2013,14(3):1118-1128
The purpose of this study was to develop taste-masked oral disintegrating tablets (ODTs) using the combination of ion exchange resin and cyclodextrin, to mask the bitter taste and enhance drug dissolution. Meloxicam (MX) was selected as a model drug with poor water solubility and a bitter taste. Formulations containing various forms of MX (free drug, MX-loaded resin or resinate, complexes of MX and 2-hydroxypropyl-β-cyclodextrin (HPβCD) or MX/HPβCD complexes, and a mixture of resinate and MX/HPβCD complexes) were made and tablets were prepared by direct compression. The ODTs were evaluated for weight variation, thickness, diameter, hardness, friability, disintegration time, wetting time, MX content, MX release, degree of bitter taste, and stability. The results showed that thickness, diameter, weight, and friability did not differ significantly for all of these formulations. The tablet hardness was approximately 3 kg/in.2, and the friability was less than 1%. Tablets formulated with resinate and the mixture of resinate and MX/HPβCD complexes disintegrated rapidly within 60 s, which is the acceptable limit for ODTs. These results corresponded to the in vivo disintegration and wetting times. However, only tablets containing the mixture of resinate and MX/HPβCD complexes provided complete MX dissolution and successfully masked the bitter taste of MX. In addition, this tablet was stable at least 6 months. The results from this study suggest that the appropriate combination of ion exchange resin and cyclodextrin could be used in ODTs to mask the bitter taste of drug and enhance the dissolution of drugs that are weakly soluble in water. 相似文献
3.
Radchatawedchakoon W. Niyomtham N. Thongbamrer C. Posa C. Sakee U. Roobsoong W. Sattabongkot J. Opanasopit P. Yingyongnarongkul B. 《Russian Journal of Bioorganic Chemistry》2020,46(3):417-428
Russian Journal of Bioorganic Chemistry - Cationic lipids with amide or carbamate linker and divalent cationic headgroups were synthesized for a transfection study. Sixteen cationic lipids with... 相似文献
4.
Involvement of serum mannan binding proteins and mannose receptors in uptake of mannosylated liposomes by macrophages 总被引:7,自引:0,他引:7
Opanasopit P Higuchi Y Kawakami S Yamashita F Nishikawa M Hashida M 《Biochimica et biophysica acta》2001,1511(1):134-145
The roles of serum mannan binding protein (MBP) and the mannose receptor in the cellular uptake of mannosylated liposomes (Man-liposomes) by macrophages were studied. Man-liposomes were prepared by incorporating cholesten-5-yloxy-N-(4-((1-imino-2-beta-D-thiomannosylethyl)amino)butyl)formamide (Man-C4-Chol) into small unilamellar long circulating liposomes consisting of cholesterol (Chol) and distearoyl phosphatidylcholine (DSPC). In the in vitro cellular uptake study with cultured mouse peritoneal macrophages, [(3)H]Man-liposomes were taken up to a great extent, whereas no significant uptake was observed for [(3)H]cholesterol and DSPC liposomes without Man-C4-Chol (Bare-liposomes). The uptake of [(3)H]Man-liposomes was dose- and temperature-dependent and inhibited by an excess of mannosylated bovine serum albumin, suggesting their specific uptake via membrane mannose receptor-mediated endocytosis. Furthermore, it was demonstrated that (111)In-MBP binds strongly to Man-liposomes based on the recognition of Man-C4-Chol and markedly enhanced their uptake by macrophages. These results are supported by confocal laser microscopic images. In addition, in vivo hepatic uptake of (111)In-MBP was enhanced by Man-liposomes. On the other hand, the uptake of Man-liposomes was significantly reduced by preincubation with serum and further with MBP-depleted serum suggesting inhibitory effects of serum proteins such as albumin on mannose receptor-mediated endocytosis. The involvement of serum-type MBP and membrane mannose receptors in the uptake of Man-liposomes is thus suggested. 相似文献
5.
Subongkot T Duangjit S Rojanarata T Opanasopit P Ngawhirunpat T 《Journal of liposome research》2012,22(3):254-262
Ultradeformable liposomes containing penetration enhancers were created to deliver NaFl. Vesicles were investigated for their particle size, zeta potential, NaFl entrapment efficiency (%EE), loading efficiency, and in vitro skin penetration. The vesicles obtained were spherical in shape, with a particle size of less than 100 nm and a negative surface charge (-6 to -11 mV). The %EE of NaFl loaded in vesicles ranged from 37 to 48%. Ultradeformable liposomes with monoterpenes (d-limonene, 1,8-cineole and geraniol) significantly improved NaFl penetration through the skin. Confocal laser scanning microscopy analysis confirmed skin-penetration results and was used to evaluate the behavior of hydrophilic compounds penetrating through the skin. 相似文献
6.
Chinsriwongkul A Chareanputtakhun P Ngawhirunpat T Rojanarata T Sila-on W Ruktanonchai U Opanasopit P 《AAPS PharmSciTech》2012,13(1):150-158
The purpose of this research was to formulate nanostructured lipid carriers (NLC) for the parenteral delivery of an anticancer
drug, all-trans retinoic acid (ATRA). The ATRA was incorporated into NLC by the de novo emulsification method. The effect of the formulation
factor, i.e., type and oil ratio, initial ATRA concentration on physicochemical properties was determined. The anticancer
efficacy of ATRA-loaded NLC on HL-60 and HepG2 cells was also studied. NLC was formulated using a blend of solid lipids (cetyl
palmitate) and liquid lipids (soybean oil (S), medium-chain triglyceride (M), S/oleic acid (O; 3:1) and M/O (3:1)) at a weight
ratio of 1:1. ATRA-loaded NLC had an average size of less than 200 nm (141.80 to 172.95 nm) with a narrow PDI and negative
zeta potential that was within an acceptable range for intravenous injection. The results indicated that oleic acid enhanced
the ATRA-loading capacity of NLC. In vitro ATRA release was only approximately 4.06% to 4.34% for 48 h, and no significant difference in ATRA release rate from all
NLC formulations in accordance with the composition of the oil phase. Moreover, no burst release of the drug was observed,
indicating that NLC could prolong the release of ATRA. The initial drug concentration affected the photodegradation rate but
did not affect the release rate. All ATRA-loaded NLC formulations exhibited the photoprotective property. The cytotoxicity
results showed that all ATRA-loaded NLC had higher cytotoxicity than the free drug and HL-60 cells were more sensitive to
ATRA than HepG2 cells. 相似文献
7.
8.
Thisirak Woraphatphadung Warayuth Sajomsang Theerasak Rojanarata Tanasait Ngawhirunpat Prasopchai Tonglairoum Praneet Opanasopit 《AAPS PharmSciTech》2018,19(3):991-1000
pH-sensitive N-naphthyl-N,O-succinyl chitosan (NSCS) and N-octyl-N,O-succinyl chitosan (OSCS) polymeric micelles carriers have been developed to incorporate curcumin (CUR) for colon-targeted drug delivery. The physical entrapment methods (dialysis, cosolvent evaporation, dropping, and O/W emulsion) were applied. The CUR-loaded micelles prepared by the dialysis method presented the highest loading capacity. Increasing initial amount of CUR from 5 to 40 wt% to polymer resulted in the increase in loading capacity of the polymeric micelles. Among the hydrophobic cores, there were no significant differences in the loading capacity of CUR-loaded micelles. The particle sizes of all CUR-loaded micelles were in the range of 120–338 nm. The morphology of the micelles changed after being contacted with medium with different pH values, confirming the pH-responsive properties of the micelles. The release characteristics of curcumin from all CUR-loaded micelles were pH-dependent. The percent cumulative release of curcumin from all CUR-loaded micelles in simulated gastric fluid (SGF) was limited to about 20%. However, the release amount was significantly increased after contacted with simulated intestinal fluid (SIF) (50–55%) and simulated colonic fluid (SCF) (60–70%). The released amount in SIF and SCF was significantly greater than the release of CUR from CUR powder. CUR-loaded NSCS exhibited the highest anti-cancer activity against HT-29 colorectal cancer cells. The stability studies indicated that all CUR-loaded micelles were stable for at least 90 days. Therefore, the colon targeted, pH-sensitive NSCS micelles may have potential to be a prospective candidate for curcumin delivery to the colon. 相似文献
9.
Jariya Kowapradit Praneet Opanasopit Tanasait Ngawhiranpat Auayporn Apirakaramwong Theerasak Rojanarata Uracha Ruktanonchai Warayuth Sajomsang 《AAPS PharmSciTech》2008,9(4):1143-1152
The aim of this study was to investigate the effect of methylated N-(4-N,N-dimethylaminobenzyl) chitosan, TM-Bz-CS, on the paracellular permeability of Caco-2 cell monolayers and its toxicity towards
the cell lines. The factors affecting epithelial permeability, e.g., degree of quaternization (DQ) and extent of dimethylaminobenzyl
substitution (ES), were evaluated in intestinal cell monolayers of Caco-2 cells using the transepithelial electrical resistance
and permeability of Caco-2 cell monolayers, with fluorescein isothiocyanate dextran 4,400 (FD-4) as a model compound for paracellular
tight-junction transport. Cytotoxicity was evaluated with the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide
viability assay. The results revealed that, at pH 7.4, TM-Bz-CS appeared to increase cell permeability in a concentration-dependent
manner, and this effect was relatively reversible at lower doses of 0.05–0.5 mM. Higher DQ and the ES caused the permeability
of FD-4 to be higher. The cytotoxicity of TM-Bz-CS depended on concentration, %DQ, and %ES. These studies demonstrated that
this novel modified chitosan has potential as an absorption enhancer. 相似文献
10.
Worranan Rangsimawong Paisit Wattanasri Prasopchai Tonglairoum Prasert Akkaramongkolporn Theerasak Rojanarata Tanasait Ngawhirunpat Praneet Opanasopit 《AAPS PharmSciTech》2018,19(5):2058-2067
The purpose of this research was to develop microemulsions (ME) and microemulgels (MG) for enhancing transdermal delivery of Kaempferia parviflora (KP) extract. The methoxyflavones were used as markers. Various formulations of ME and MG containing 10% w/v KP extract were prepared, and the in vitro skin permeation and deposition were investigated. The potential ME system containing oleic acid (5% w/v), Tween 20 (20% w/v), PG (40% w/v), and water (35% w/v) was successfully formulated. ME with 10% w/v limonene (ME-L10%) showed higher methoxyflavones flux than ME-L5%, ME-L1%, ME without limonene, and KP extract in water, respectively. ME-L10% was selected for adding a gelling agent to form microemulgels (MG-L10%). However, the high viscosity of the gel formulation might control the diffusion of the compound from gel layer into the skin. Therefore, the liquid formulation provided potential ME droplets to deliver KP extract through the skin. Limonene also plays an effective role on the skin permeation, in which the histological image of the skin treated with ME-L10% exhibited larger space of each flattened keratinocyte layer in the stratum corneum compared to the skin treated with KP extract in water. Moreover, ME-L10% showed good stability. Therefore, ME-L10% was a potential formulation for improving transdermal delivery of KP extract. 相似文献