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Hydrogels were synthesized as the drug reservoir matrix for peptide-based pharmaceuticals, and the iontophoretic release and transdermal delivery of three model peptides, insulin, calcitonin, and vasopressin, from these hydrogel-based iontotherapeutic devices were investigated. The swelling behavior of polyacrylamide-type hydrogel as a function of its monomer and cross-linker concentration was studied, and a hydrogel with minimal swelling was synthesized. The release of peptides from the hydrogel matrix was found to follow a Q vs t
1/2 relationship under passive diffusion conditions, which shifted to a Q vs t relationship under iontophoresis-facilitated transport. The release flux (dQ/dt) of peptides was observed to decline when the electric current was turned off and was resumed when the current was turned on, thus allowing for modulation of drug release by varying the application parameters of iontophoresis-facilitated transport. The permeability coefficients for these peptides across the hairless rat skin were evaluated using the hydrogel formulations prepared from polyacrylamide, p-HEMA, and carbopol. A rank order of vasopressin > calcitonin > insulin was obtained in accordance with the order of molecular size. 相似文献
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目的: 了解国内外对于可溶性聚合物微针这一新型药物递送系统的研究进展,并对其优势及存在的问题进行分析,对发展前景进行展望。方法: 通过文献调研,总结可溶性聚合物微针的材料及功能,分析可溶性微针所解决的临床用药问题,以及各微针基质材料所具有的优势与面临的挑战。结果: 本文以临床不同的用药需求为视角进行分类,介绍了聚合物材料在可溶性微针递药系统中的应用,并对其优势及面临的挑战进行总结,对发展前景进行展望。结论: 目前对于可溶性聚合物微针的研究已取得了令人瞩目的进展。然而,为实现临床转化,可溶性聚合物微针递药系统的载药能力、安全性等方面仍然需要进一步的研究。 相似文献
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Meilin He Guozhong Yang Suohui Zhang Xiaoyu Zhao Yunhua Gao 《Journal of pharmaceutical sciences》2018,107(4):1037-1045
The study design is that lipophilic drug was encapsulated within dissolving microneedles (DMNs) for sustained-release delivery over 1 week. Etonogestrel (ENG), the progestogen used in hormonal contraceptives, was loaded in 2-layered DMNs in the form of microcrystal particles (MPs). In vitro release study indicated that ENG in the MP form could sustain drug release compared to noncrystal form. Hydroxypropyl methylcellulose and polyvinyl alcohol were used to prepare the fast dissolving needle tips and flexible back layer, respectively. The mechanical strength of microneedles was not affected even with the drug-loading efficiency of 50.0% in needle tips. The penetration depth of DMNs in skin, observed using a confocal laser scanning microscope, was approximately 280 μm. The tips of DMNs could be dissolved in rat skin within 1 h with a drug delivery efficiency of 63.8 ± 2.0%. The pharmacokinetic study of DMN treatment in rats showed that the plasma levels of ENG were a dose-dependent profile and were much steadier than intradermal (ID) injections. There was no statistical difference between bioavailability of ENG treated with DMNs or ID injections (p >0.05). Therefore, the novel DMNs loaded with drug MP provided a potential minimally invasive route for ID sustained delivery of lipophilic drug. 相似文献
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《Journal of pharmaceutical sciences》2019,108(11):3649-3656
This study focuses on the in vitro transdermal transport of sumatriptan succinate using combined iontophoresis and dissolving polymeric microneedle arrays. Permeation experiments were performed to evaluate the effects of formulation parameters on drug release from polyvinylpyrrolidone systems under mild electrical current (≤500 μA/cm2). The preparations consisted of hydrophilic, positively charged molecules encapsulated in a water-soluble and biocompatible polymeric material. Current densities of 100, 300, and 500 μA/cm2 were applied during a 6-h period using silver/silver chloride electrodes. The circular array consisted of 600 needles and occupied a 0.785 cm2 area. Tests, carried out with Franz diffusion cells and skin of Göttingen minipigs, showed that small decreases in the polymer concentration led to negligible lag times and marked increases in the cumulative amount of drug permeated in 6 h (Q6h) and in the flux (Jss). At 500 μA/cm2, Q6h and Jss nearly doubled for a microneedle loaded with 5% (w/w) sumatriptan and 20% (w/w) PVP (lag time = 0 min; Q6h = 2888 μg/cm2; Jss = 490 μg/cm2/h) relative to a system loaded with 5% (w/w) drug and 30% (w/w) PVP (lag time = 36 min; Q6h = 1437 μg/cm2; Jss = 266 μg/cm2/h). 相似文献
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多肽、蛋白质药物鼻腔给药系统的研究进展 总被引:2,自引:0,他引:2
随着生物技术和遗传工程的发展,多肽与蛋白质类药物的种类及数量日益增多,临床应用越来越广泛,相应的制剂学研究也日益受到重视。常见的多肽和蛋白质类药物如血管紧张素Ⅱ抑制剂、心房肽激素、脑啡肽、人生长激素(hGH)、免疫调节系统药物如集落刺激因子、代谢调节系统药物如胰岛素等, 相似文献
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Fabrication of Rapidly Separable Microneedles for Transdermal Delivery of Metformin on Diabetic Rats
《Journal of pharmaceutical sciences》2021,110(8):3004-3010
In this work, the rapidly separable microneedles (MNs) consisted of needle-tips and supporting bases have been fabricated by a step-by-step coating method. Poly (vinyl alcohol) (PVA) have been used to prepare the needle-tips of MNs in which they are capped on the solvable supporting bases consisted of sodium bicarbonate, poly (vinyl pyrolidone) (PVP), and tartaric acid (TA) (NaHCO3/PVP/TA). After insertion into the skin, the needle-tips can be separated rapidly from the patches within 90 s due to the generation of air bubbles in the supporting bases by the reaction between NaHCO3 and TA after absorption of tissue fluid, leading to the needle-tips remaining in the skin tissue. Metformin, a hypoglycemic drug, encapsulated in the needle-tips of MNs can be released due to swelling and decomposition of PVA by the absorption of tissue fluid. To investigate the pharmacological effect via transdermal delivery route, metformin-loaded MNs are applied on the diabetic SD rats induced by streptozotocin (STZ). They exhibit a longer hypoglycemic effect in vivo than that of subcutaneous injection. These results indicated the as-fabricated rapidly separable MNs present a promising platform for transdermal delivery of drugs against diabetic patients. 相似文献
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纳米粒作为肽类和蛋白质类药物的载体 总被引:3,自引:0,他引:3
用纳米粒作为肽类和蛋白质药物的载体可以有效地克服肽类和蛋白质类药物在体内稳定性差、吸收不佳、半衰期短等缺陷,从而显著地增强疗效。本文从制备方法、体内吸收、药效学等三方面对近年来这一领域的研究进展进行综述,并介绍了最新的研究动向。 相似文献
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Leonard Y. Chu Seong-O. Choi Mark R. Prausnitz 《Journal of pharmaceutical sciences》2010,99(10):4228-4238
Dissolving microneedle patches offer promise as a simple, minimally invasive method of drug and vaccine delivery to the skin that avoids the need for hypodermic needles. However, it can be difficult to control the amount and localization of drug within microneedles. In this study, we developed novel microneedle designs to improve control of drug encapsulation and delivery using dissolving microneedles by (i) localizing drug in the microneedle tip, (ii) increasing the amount of drug loaded in microneedles while minimizing wastage, and (iii) inserting microneedles more fully into the skin. Localization of our model drug, sulforhodamine B in the microneedle tip by either casting a highly concentrated polymer solution as the needle matrix or incorporating an air bubble at the base of the microneedle achieved approximately 80% delivery within 10 min compared to 20% delivery achieved by the microneedles encapsulating nonlocalized drug. As another approach, a pedestal was introduced to elevate each microneedle for more complete insertion into the skin and to increase its drug loading capacity by threefold from 0.018 to 0.053 μL per needle. Altogether, these novel microneedle designs provide a new set of tools to fabricate dissolving polymer microneedles with improved control over drug encapsulation, loading, and delivery. 相似文献
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Polymer Microneedles for Controlled-Release Drug Delivery 总被引:5,自引:0,他引:5
Purpose As an alternative to hypodermic injection or implantation of controlled-release systems, this study designed and evaluated
biodegradable polymer microneedles that encapsulate drug for controlled release in skin and are suitable for self-administration
by patients.
Methods Arrays of microneedles were fabricated out of poly-lactide-co-glycolide using a mold-based technique to encapsulate model drugs—calcein and bovine serum albumin (BSA)—either as a single
encapsulation within the needle matrix or as a double encapsulation, by first encapsulating the drug within carboxymethylcellulose
or poly-l-lactide microparticles and then encapsulating drug-loaded microparticles within needles.
Results By measuring failure force over a range of conditions, poly-lactide-co-glycolide microneedles were shown to exhibit sufficient mechanical strength to insert into human skin. Microneedles were
also shown to encapsulate drug at mass fractions up to 10% and to release encapsulated compounds within human cadaver skin.
In vitro release of calcein and BSA from three different encapsulation formulations was measured over time and was shown to be controlled
by the encapsulation method to achieve release kinetics ranging from hours to months. Release was modeled using the Higuchi
equation with good agreement (r2 ≥ 0.90). After microneedle fabrication at elevated temperature, up to 90% of encapsulated BSA remained in its native state,
as determined by measuring effects on primary, secondary, and tertiary protein structure.
Conclusions Biodegradable polymer microneedles can encapsulate drug to provide controlled-release delivery in skin for hours to months. 相似文献
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HITOSHI SASAKI MASATAKA ICHIKAWA KENZO YAMAMURA KOYO NISHIDA JUNZO NAKAMURA 《The Journal of pharmacy and pharmacology》1997,49(2):135-139
The purpose of this study is to investigate the ocular membrane permeability and the permeation mechanism of hydrophilic drugs such as thyrotropin-releasing hormone (TRH), p-nitrophenyl β-cellopentaoside (PNP) and luteinizing hormone-releasing hormone (LHRH). The penetration of hydrophilic drugs was measured across the isolated corneal and conjunctival membranes of albino rabbits using a two-chamber diffusion glass cell. The corneal permeabilities of hydrophilic drugs were much lower than those of beta blockers reported previously. The corneal penetration of TRH was the highest among the hydrophilic drugs studied. Scraping the corneal epithelium increased the penetration of hydrophilic drugs. Conjunctival membranes showed higher permeability to hydrophilic drugs compared with corneal membranes. The permeability of drugs was also analysed by Fick's equation. The partition parameter and diffusion parameter of TRH, PNP and LHRH in the cornea were lower than those in scraped cornea and conjunctiva. In addition to the data of fluorescein isothiocyanate-dextran reported previously, the permeability coefficient of hydrophilic drugs through the cornea, scraped cornea and conjunctiva correlated with molecular weight of the drugs. The diffusion parameters of hydrophilic drugs decreased with an increase of molecular weight for all ocular membranes. The extent of dependency of partition parameters on the molecular weights of drugs varied according to the ocular membrane. These results indicate that ocular membranes are sufficiently different in permeation character and mechanism to control the extent and pathway for ocular absorption of hydrophilic drugs. 相似文献
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Chitosan as a Novel Nasal Delivery System for Peptide Drugs 总被引:16,自引:0,他引:16
A nasal solution formulation of the cationic material chitosan was shown to greatly enhance the absorption of insulin across the nasal mucosa of rat and sheep. The absorption promoting effect was concentration dependent with the optimal efficacy obtained for concentrations higher than 0.2% and 0.5% in rats and sheep, respectively. The absorption promoting effect was reversible with time in a pulse-chase study. Histological examination of the nasal mucosa of rats exposed to a chitosan solution for 60 minutes showed little change. 相似文献
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蛋白和多肽药物的透粘膜吸收 总被引:4,自引:0,他引:4
随着蛋白和多肽药物的增多,其非注射给药剂型的研究受到了越来越多的重视,本文综述了国外对鼻腔、口腔、口服、直肠和阴道几种主要透粘膜吸收给药途径的研究。蛋白和多肽药物的透粘膜给药剂型的研究推进了蛋白和多肽药物的临床应用。 相似文献
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《Journal of pharmaceutical sciences》2022,111(10):2867-2878
Microneedles are used to deliver drugs topically across the skin and mucous membranes. Dissolvable microneedles are made using soluble polymers, which disintegrates in the tissue and release the entire payload instantaneously including the polymer construct. Often, a slow release of drug into the tissue is desirable to overcome the severity of side effects at the site of administration as well as systemic adverse effects. In addition, controlled release of active pharmaceutical ingredient (API) only (not the excipients) is safe and effective particularly when the drug delivery is intended to sensitive organs like the eye. In this project, the feasibility of fabricating polymer coated polymeric (PCP) microneedles to achieve a gradual release of only the active ingredient from the device was investigated. The potential application of such PCP microneedles in the dermal and intravitreal drug delivery was also explored using animal tissue models. The PCP microneedles were found to be intact even after prolonged contact with the release medium. The time at which 50% (T50%) of dextran (10 K) was released in case of microneedles prepared using 20% of core polymer (PVP-K30) was about 15 min versus less than 5 min in the case of uncoated microneedles. Whereas when the core polymer concentration was increased to 50%, the T50% was increased to 90 min. The rate of release depended on the polymer molecular weight grade. The rate of drug release was not influenced by the total amount of concentration of dextran. The PCP microneedles of lidocaine hydrochloride could constantly release the drug for up to 9 h in the skin tissue. Likewise, the PCP microneedles infused voriconazole, intravitreally for 6 h. 相似文献