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71.
72.
Cyclosporine A-nanosuspensions were prepared using zirconium oxide beads as a milling media, Poloxamer 407 as a stabilizer and distilled water as an aqueous medium using the Pearl Milling technique. The optimized formulation was characterized in terms of particle size distribution, surface morphology, drug-surfactant interaction, drug content, saturation solubility, osmolarity, and stability. The nanoparticles consisting of Poloxamer-bound cyclosporin A with a mean diameter of 213 nm revealed a spherical shape and 5.69 fold increased saturation solubility as compared to the parent drug. The formulation was found to be iso-osmolar with blood and stable up to 3 months at 2–8°C. In-vivo studies were carried out in albino rats and the pharmacokinetic parameters were compared with a marketed formulation, which indicated better results of the prepared formulation than the marketed one. 相似文献
73.
Hee Jun Choi Jai Min Ryu Byung Joo Chae Eun-Kyu Kim Jun Won Min Hyuk Jai Shin Seok Jin Nam Jonghan Yu Jeong Eon Lee Se Kyung Lee Seok Won Kim 《JOURNAL OF BREAST CANCER》2021,24(4):367
PurposeRestricted shoulder motion is a major morbidity associated with a lower quality of life and disability after axillary lymph node dissection (ALND) in patients with breast cancer. This study sought to evaluate the antiadhesive effect of a poloxamer-based thermosensitive sol-gel (PTAS) agent after ALND.MethodsWe designed a double-blind, multicenter randomized controlled study to evaluate the clinical efficacy and safety of PTAS in reducing upper-limb dysfunction after ALND. The primary outcome was the change in the range of motion (ROM) of the shoulder before surgery and 4 weeks after ALND (early postoperative period). Secondary outcomes were shoulder ROM at six months, axillary web syndrome, and lymphedema (late postoperative period).ResultsA total of 170 patients with planned ALND were randomly assigned to one of 2 groups (poloxamer and control) and 15 patients were excluded. In the poloxamer group (n = 76), PTAS was applied to the surface of the operative field after ALND. ALND was performed without the use of poloxamer in the control group (n = 79). Relative to the control group, the poloxamer group had significantly lower early postoperative restrictions in total shoulder ROM at four weeks (−30.04 ± 27.76 vs. −42.59 ± 36.79; p = 0.0236). In particular, the poloxamer group showed greater reductions in horizontal abduction at four weeks (−3.92 ± 9.80 vs. −10.25 ± 15.42; p = 0.0050). The ROM of the shoulder at 24 weeks, axillary web syndrome, and lymphedema were not significantly different between the two groups. No adverse effects were observed in either group.ConclusionWe suggest that poloxamer might improve the early postoperative shoulder ROM in patients with breast cancer who have undergone ALND.Trial RegistrationClinicalTrials.gov Identifier: NCT02967146相似文献
74.
Effect of various poloxamer coatings on in vitro adhesion of isohexylcyanoacrylate nanospheres to rat ileal segments under liquid flow 总被引:3,自引:0,他引:3
Clara Pimienta Fran ois Chouinard Akbiri Labib Vincent Lenaerts 《International journal of pharmaceutics》1992,80(1-3):1-8
This work evaluates the bioadhesive properties of isohexylcyanoacrylate nanocapsules coated with poloxamers 407, 238, 403 and poloxamine 908 compared to nanoparticles coated with poloxamer 407. Nanocapsules (oil droplets surrounded by a polymeric wall) and nanoparticles (plain polymeric spheres) were prepared, labelled with covalently linked with tetraiodinated 125I-phthalocyanine-Zn and laid on the rat ileal segment in vitro. After 0 and 10 min following transfer of nanospheres, a liquid flow was started. In all cases studied, a fraction of the nanospheres was not adherent when perfusion was initiated and was recovered in the first fraction. The other fraction, representing approx. 45% of the nanospheres, adhered firmly and was removed very slowly by the liquid flow. In addition, when nanocapsules were coated with poloxamers 238 and 407, the percentage adhesion increased between and 10 min. Our results demonstrate that the greatest extent of mucoadhesion was achieved with poloxamers possessing a short centra polyoxypropylene (POP) chain and long polyoxyethylene (POE) side chains. The results are discussed on the basis of diffusion of the POE groups into the mucin network and creation of secondary chemical adhesive bonds (Van der Waals type) between the nanosphere coating and mucus. 相似文献
75.
Torsten M. Gppert Rainer H. Müller 《European journal of pharmaceutics and biopharmaceutics》2005,60(3):361-372
Solid lipid nanoparticles (SLN) were produced using a full range of poloxamer polymers and poloxamine 908 for stabilization. The protein adsorption pattern acquired on the surface of these particles after intravenous injection is the key factor determining the organ distribution. Two-dimensional polyacrylamide gel electrophoresis (2-DE) was employed for determination of particle interactions with human plasma proteins. The objective of this study was to investigate changes in the plasma protein adsorption patterns in the course of variation of the polymers stabilizing the SLN. Considerable differences in the protein adsorption with regard to preferential adsorbed proteins were detected for the different stabilizers. Possible correlations between the polyethylene oxide (PEO) chain length and the adsorption of various proteins (first of all apolipoproteins) are shown and discussed. Besides the study of protein adsorption patterns, the total protein mass adsorbed to the SLN was also evaluated using the bicinchoninic acid (BCA)-protein assay. The knowledge concerning the interactions of proteins and nanoparticles can be used for a rational development of particulate drug carriers. Based on the findings presented in this paper, we anticipate that the in vivo well-tolerable SLN are a promising site-specific drug delivery system for intravenous injection. 相似文献
76.
利巴韦林鼻用温敏凝胶热力学和流变学性质研究 总被引:4,自引:1,他引:4
考察了不同浓度泊洛沙姆407、PEG6000和泊洛沙姆188及处方量利巴韦林对鼻用温敏凝胶的热力学[胶凝温度(T1)、胶融温度(T2)]和流变学性质(黏度)的影响。结果表明,凝胶的T1和黏度均与泊洛沙姆407浓度呈负相关,而T2则与其呈正相关;利巴韦林和相应辅料对凝胶的T1、T2和黏度都有不同程度的影响。 相似文献
77.
Urbán-Morlán Z Castro-Ríos R Chávez-Montes A Melgoza-Contreras LM Piñón-Segundo E Ganem-Quintanar A Quintanar-Guerrero D 《Journal of pharmaceutical and biomedical analysis》2008,46(4):799-803
Poloxamers (PXMs) are amphiphilic non-ionic block polymers commonly used in the cosmetic and pharmaceutical industries. In spite of the wide use of PXMs, few studies have dealt with the analysis of these polymers in pharmaceutical preparations. In this work, high-performance thin-layer chromatography (HPTLC) has been used to quantify both PXM-188 and PXM-407 in pharmaceutical preparations. The separation of these compounds was carried out using reverse phase HPTLC plates with a chloroform-methanol mixture as the mobile phase. Detection was performed densitometrically using the Dragendorff's reagent for the visualization of PXMs. Quality parameters were established, and the detection limits ranged from 24 to 47ng/spot. A good precision (day to day and run to run), with relative standard deviations <11.18%, was obtained. The proposed method was satisfactorily applied to the analysis of laboratory-made and commercial pharmaceutical products. 相似文献
78.
目的:观察三氧化二砷-泊洛沙姆407(As2O3-P407)缓释剂对裸鼠皮下人肝癌移植瘤的有效性。方法:以人肝癌HepG2细胞为来源建立裸鼠皮下移植瘤模型,实验共分3组:As2O3-P407缓释剂治疗组、As2O3治疗组和生理盐水(NS)对照组,于造模成功后6~8天行瘤体注射,每4天1次,共4次。比较各组抗癌疗效,观察裸鼠体重、肿瘤体积变化、抑瘤率、肿瘤组织病理及骨髓涂片以及裸鼠的存活情况、生存质量。结果:As2O3 P407缓释剂治疗组肿瘤生长受到显著抑制,肿瘤体积较As2O3组小(P<0.05),瘤重分别为(0.257±0.080)g和(0.641±0.109)g,差异有统计学意义(P<0.05);两组与NS对照组瘤重(1.094±0.147)g相比,差异有统计学意义(P<0.05)。治疗后As2O3-P407缓释剂组裸鼠体重大于As2O3组和NS对照组,差异有统计学意义(P<0.05)。各组均未见骨髓抑制现象。结论:As2O3-P407缓释剂瘤内注射,使用安全,可维持局部有效药物浓度、延长作用时间,疗效优于As2O3注射液。 相似文献
79.
穿心莲有效部位Poloxamer188聚合物胶束的制备工艺 总被引:1,自引:0,他引:1
目的制备Poloxamer188穿心莲有效部位的聚合物胶束。方法薄膜水化法制备穿心莲有效部位聚合物胶束,正交设计优化处方工艺。HPLC法测定其载药量和包封率,激光粒度仪测定粒径。结果载药胶束包封率为(85.7+2.1)%,载药量为(1.11+0.09)%,粒径为(198.32+3.35)nm。结论载药Poloxamer188胶束制备工艺简便易行,为中药制剂提供了新剂型。 相似文献
80.
M.S. Espuelas P. Legrand P.M. Loiseau C. Bories G. Barratt J.M. Irache 《Journal of drug targeting》2013,21(8):593-599
The activity of formulations for amphotericin B (AmB) associated with poly (ε -caprolactone) nanospheres and coated with variable amounts of a non ionic surfactant poloxamer 188, was evaluated against AmB-susceptible (WT) and AmB-resistant (AmB r) strains of Leishmania donovani amastigotes in thioglycolate-elicited peritoneal macrophages. AmB-nanospheres were more actives than free AmB only against amastigotes of wild strain. The activity was not influenced by the concentration of poloxamer 188 used to stabilize the nanospheres in spite of this surfactant was previously reported to synergy with AmB on the membrane of the resistant parasite. Similarly, this improvement was not mediated through macrophage activation. In fact, these nanoparticle formulations appeared to inhibit both NO and TNF- α production induced by the free drug. Therefore, we suggest that the association of AmB with nanospheres may improve the capability of the drug to interact with ergosterol. This hypothesis appears to be supported by the fact that nanospheres did not show any improvement of the AmB activity against the resistant strain (characterized by the absence of ergosterol). 相似文献