Preparation and Properties of 5-Fluorouracil-Loaded Chitosan Microspheres for the Intranasal Administration

Li, Wanqing; Ba, Hongyuan; Huang, Peng; Zheng, Aiping; Yang, Xi

doi:10.1055/a-0586-8406

Cited by 11 publications

(3 citation statements)

References 19 publications

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“…Although both PTX EtOH - and PTX nano -GP-MS were able to prolong the residence time of PTX in the abdominal cavity, PTX nano -GP-MS were more efficacious in eradicating minimal peritoneal disease and preventing recurrent peritoneal carcinomatosis. It has already been reported that PTX nanocrystals demonstrate a high cellular uptake due to their size and accumulate in tumor tissue, increasing the efficacy of PTX therapy 13,61,62 .…”

Section: Discussionmentioning

confidence: 99%

Preclinical evaluation of local prolonged release of paclitaxel from gelatin microspheres for the prevention of recurrence of peritoneal carcinomatosis in advanced ovarian cancer

Clercq

Xie

Wever

et al. 2019

Sci Rep

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Patients with advanced ovarian cancer develop recurrence despite initial treatment response to standard treatment of surgery and intravenous/intraperitoneal (IP) chemotherapy, partly due to a limited peritoneal exposure time of chemotherapeutics. Paclitaxel-loaded genipin-crosslinked gelatin microspheres (PTX-GP-MS) are evaluated for the treatment of microscopic peritoneal carcinomatosis and prevention of recurrent disease. The highest drug load (39.2 µg PTX/mg MS) was obtained by immersion of GP-MS in aqueous PTX nanosuspension (PTXnano-GP-MS) instead of ethanolic PTX solution (PTXEtOH-GP-MS). PTX release from PTX-GP-MS was prolonged. PTXnano-GP-MS displayed a more controlled release compared to a biphasic release from PTXEtOH-GP-MS. Anticancer efficacy of IP PTX-GP-MS (PTXEtOH-GP-MS, D = 7.5 mg PTX/kg; PTXnano-GP-MS D = 7.5 and 35 mg PTX/kg), IP nanoparticular albumin-bound PTX (D = 35 mg PTX/kg) and controls (0.9% NaCl, blank GP-MS) was evaluated in a microscopic peritoneal carcinomatosis xenograft mouse model. PTXnano-GP-MS showed superior anticancer efficacy with significant increased survival time, decreased peritoneal carcinomatosis index score and ascites incidence. However, prolonged PTX release over 14 days from PTXnano-GP-MS caused drug-related toxicity in 27% of high-dosed PTXnano-GP-MS-treated mice. Dose simulations for PTXnano-GP-MS demonstrated an optimal survival without drug-induced toxicity in a range of 7.5–15 mg PTX/kg. Low-dosed PTXnano-GP-MS can be a promising IP drug delivery system to prevent recurrent ovarian cancer.

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Section: Discussionmentioning

confidence: 99%

Preclinical evaluation of local prolonged release of paclitaxel from gelatin microspheres for the prevention of recurrence of peritoneal carcinomatosis in advanced ovarian cancer

Clercq

Xie

Wever

et al. 2019

Sci Rep

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“…As reported in the literature [ 9 , 24 , 35 ], 50 mg of aerogel was accurately weighed and placed in 50 mL HCl aqueous solution (pH = 1) and desorption of 5-Fu occurred at 60 °C for 3 h. Next, the absorbance of 1 mL of filtrate was measured at 265 nm. The drug loading (DL) and encapsulation efficiency (EE) were calculated using the following equation: DL = [Drug loading/(Drug loading + Aerogel)] × 100% EE = (Determined drug loading/(Theoretic drug loading) × 100% …”

Section: Methodsmentioning

confidence: 99%

Fabrication and Evaluation of Graphene Oxide/Hydroxypropyl Cellulose/Chitosan Hybrid Aerogel for 5-Fluorouracil Release

Sang

Miao

Chen

et al. 2022

Gels

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The incorporation of graphene oxide (GO) into a polymeric drug carrier can not only enhance the loading efficiency but also reduce the initial burst and consequently improve the controllability of drug release. Firstly, 5-fluorouracil (5-Fu)-loaded hydroxypropyl cellulose/chitosan (HPC/CS@5-Fu) and GO/HPC/CS@5-Fu aerogels were successfully fabricated through chemical cross-linking with glutaraldehyde. Then, the obtained aerogels were characterized using scanning electron microscopy (SEM), Fourier transform infrared (FITR), X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermogravimetry (TG), and the effect of HPC and GO content on the drug loading (DL) and encapsulation efficiency (EE) for the two aerogels were investigated, respectively. Finally, the drug release behavior of the GO/HPC/CS@5-Fu aerogels with different GO content was evaluated at two different pH values, and four kinds of kinetic models were used to evaluate the release behavior.

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“…In recent times, microsphere formulations have achieved tremendous significance as oral drug delivery systems due to predictable gastric emptying, reduced local irritation and fewer toxic effects as compared to unit dosage forms which make these systems more preferable. Chitosan has been used as an ex-cipient of choice in formulating biodegradable microspheres owing to its property of modifying the drug release and also exerting mucoadhesive effect [1][2][3]. Since the matrices made of cross-linked chitosan amicably alter the release of a loaded drug, so the current study endeavored the determination of effect of diverse cross-linking agents on the release of drug loaded in chitosan microspheres.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Characterization of Losartan Loaded Chitosan Microspheres: Effect of Crosslinking Agents

2020

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Objective The present investigation entailed determination of effect of diverse cross-linking agents on Losartan Potassium loaded chitosan microspheres. The emulsion cross-linking method was employed to formulate the microspheres with an endeavour to achieve maximum sustained effect. Methods The FTIR studies revealed absence of any interaction between Losartan and chitosan. The emulsion cross linking method was accomplished in three steps encompassing formation of an aqueous and oily phase, emulsification and cross-linking. A total of eighteen Losartan formulations were developed using six different cross-linkers at three varying level were screened for optimum parameters. The in vitro drug release parameters of optimum formulations (LC3, LE3, LF3, LG3, LS3 and LV3) containing citric acid, epichlorohydrin, formaldehyde, glutaraldehyde, suphuric acid and vanillin as cross-linkers were assessed to determine the sustained effect. Results The values of evaluated parameters including percent yield (94.67%), average particle size (51.19 µm), drug content (44.38 mg) and entrapment efficiency (88.77%) connoted LG3 as the best formulation. Additionally, the values of relative measure of skewness (β1=0.01 and γ1=0.10) and platykurtic (β2=1.26) size distribution were least for LG3 with spherical shape and smooth surface as revealed by SEM studies. Conclusion The outcome of in vitro release and other characterizations of microspheres explicitly revealed glutaraldehyde as the best cross-linker amongst the cross-linkers used herewith. The maximum sustained effect (lasting over a period of 24 h) accompanied with higher MDT and t50% with lower%DE and Q14h values thus corroborated the objective of attaining sustained release of Losartan.

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Preparation and Properties of 5-Fluorouracil-Loaded Chitosan Microspheres for the Intranasal Administration

Cited by 11 publications

References 19 publications

Preclinical evaluation of local prolonged release of paclitaxel from gelatin microspheres for the prevention of recurrence of peritoneal carcinomatosis in advanced ovarian cancer

Preclinical evaluation of local prolonged release of paclitaxel from gelatin microspheres for the prevention of recurrence of peritoneal carcinomatosis in advanced ovarian cancer

Fabrication and Evaluation of Graphene Oxide/Hydroxypropyl Cellulose/Chitosan Hybrid Aerogel for 5-Fluorouracil Release

Formulation and Characterization of Losartan Loaded Chitosan Microspheres: Effect of Crosslinking Agents

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