Preparation of Amphiphilic Chitosan Nanoparticles for Controlled Release of Hydrophobic Drugs

Background: The purpose of this study was to formulate, characterize and in-vitro cytotoxicity of 5-Fluorouracil loaded controlled release nanoparticles for the treatment of skin cancer. The patents on nanoparticles (US8414926B1), (US61654404A), (WO2007150075A3) etc. helped in the selection polymers and method for the preparation of nanoparticles. Methods: In the present study nanoparticles were prepared by simple ionic gelation method using various concentrations of chitosan and sodium tripolyphosphate (TPP). Several process and formulation parameters were screened and optimized using 25-2 fractional factorial design. The prepared nanoparticles were evaluated for particle size, shape, charge, entrapment efficiency, crosslinking mechanism and drug release study. Results: The optimized 5-Fluorouracil loaded nanoparticle were found with particle size of of 320±2.1 nm, entrapment efficiency of 85.12%± 1.1% and Zeta potential of 29mv±1mv. Scanning electron microscopy and dynamic light scattering technique revealed spherical particles with uniform size. The invitro release profile showed controlled release up to 24 hr. Further study was carried using A375 basal cell carcinoma cell-line to elucidate the mechanism of its cytotoxicity by MTT assay. Conclusion: These results demonstrate that the possibility of delivering 5-Fluorouracil to skin with enhanced encapsulation efficiency indicating effectiveness of the formulation for treatment of basal cell carcinoma type of skin cancer.

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DEVELOPMENT AND CHARACTERIZATION OF CHITOSAN NANOPARTICLES LOADED NANOFIBER HYBRID SYSTEM FOR VAGINAL CONTROLLED RELEASE OF BENZYDAMINE

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2021.105801 ◽

2021 ◽

pp. 105801

Author(s):

Fatmanur Tuğcu-Demiröz ◽

Sinem Saar ◽

Adnan Altuğ Kara ◽

Ayşegül Yıldız ◽

Emre Tunçel ◽

...

Keyword(s):

Controlled Release ◽

Hybrid System ◽

Chitosan Nanoparticles

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Controlled release of turmeric oil from chitosan nanoparticles extends shelf life of Agaricus bisporus and preserves its postharvest quality

Food Bioscience ◽

10.1016/j.fbio.2021.101401 ◽

2021 ◽

Vol 44 ◽

pp. 101401

Author(s):

Masomeh Valizadeh ◽

Mahdi Behnamian ◽

Sara Dezhsetan ◽

Roghayeh Karimirad

Keyword(s):

Controlled Release ◽

Shelf Life ◽

Agaricus Bisporus ◽

Chitosan Nanoparticles ◽

Postharvest Quality

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Molecular simulation and in vitro evaluation of chitosan nanoparticles as drug delivery systems for the controlled release of anticancer drug cytarabine against solid tumours

3 Biotech ◽

10.1007/s13205-018-1510-x ◽

2018 ◽

Vol 8 (12) ◽

Cited By ~ 3

Author(s):

G. Deepa ◽

K. C. Sivakumar ◽

T. P. Sajeevan

Keyword(s):

Drug Delivery ◽

Controlled Release ◽

Molecular Simulation ◽

Anticancer Drug ◽

Drug Delivery Systems ◽

Chitosan Nanoparticles ◽

Delivery Systems ◽

Solid Tumours ◽

In Vitro Evaluation

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Effective protection and controlled release of insulin by cationic β-cyclodextrin polymers from alginate/chitosan nanoparticles

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2010.04.006 ◽

2010 ◽

Vol 393 (1-2) ◽

pp. 213-219 ◽

Cited By ~ 127

Author(s):

Nan Zhang ◽

Jiahui Li ◽

Wenfeng Jiang ◽

Chunhong Ren ◽

Jianshu Li ◽

...

Keyword(s):

Controlled Release ◽

Chitosan Nanoparticles ◽

Effective Protection ◽

Cyclodextrin Polymers

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Magnetically controlled release of recombinant tissue plasminogen activator from chitosan nanocomposites for targeted thrombolysis

Journal of Materials Chemistry B ◽

10.1039/c5tb02579f ◽

2016 ◽

Vol 4 (15) ◽

pp. 2578-2590 ◽

Cited By ~ 18

Author(s):

Jyh-Ping Chen ◽

Chih-Hsin Liu ◽

Hao-Lung Hsu ◽

Tony Wu ◽

Yu-Jen Lu ◽

...

Keyword(s):

Controlled Release ◽

Plasminogen Activator ◽

Tissue Plasminogen Activator ◽

Targeted Delivery ◽

Chitosan Nanoparticles ◽

Recombinant Tissue Plasminogen Activator ◽

Triggered Release ◽

Magnetic Chitosan ◽

Tissue Plasminogen ◽

Thrombolysis Therapy

Targeted delivery and triggered release of rtPA-encapsulated magnetic chitosan nanoparticles with the guidance of a magnet could be used for remote-controlled thrombolysis therapy.

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Electrospun poly(NVCL-co-AA) fibers as potential thermo-and pH-sensitive agents for controlled release of hydrophobic drugs

Materials Science and Engineering B ◽

10.1016/j.mseb.2021.115531 ◽

2022 ◽

Vol 276 ◽

pp. 115531

Author(s):

Marwa Sta ◽

Dayane B. Tada ◽

Simone F. Medeiros ◽

Amilton M. Santos ◽

Nicole R. Demarquette

Keyword(s):

Controlled Release ◽

Ph Sensitive ◽

Hydrophobic Drugs

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Synthesis, Characterization, and Evaluation of Genistein-Loaded Zein/Carboxymethyl Chitosan Nanoparticles with Improved Water Dispersibility, Enhanced Antioxidant Activity, and Controlled Release Property

Foods ◽

10.3390/foods9111604 ◽

2020 ◽

Vol 9 (11) ◽

pp. 1604

Author(s):

Yu Xiao ◽

Chi-Tang Ho ◽

Yulian Chen ◽

Yuanliang Wang ◽

Zihao Wei ◽

...

Keyword(s):

Antioxidant Activity ◽

Controlled Release ◽

Water Solubility ◽

Uv Light ◽

Chitosan Nanoparticles ◽

Carboxymethyl Chitosan ◽

Food Ingredient ◽

Beneficial Effects ◽

Release Property ◽

Water Dispersibility

Genistein is one of major isoflavones derived from soybean products and it is believed to have beneficial effects on human health. However, its low water-solubility and poor oral bioavailability severely hamper its use as a functional food ingredient or for pharmaceutical industry. In this study, zein and zein/carboxymethyl chitosan (CMCS) nanoparticles were prepared to encapsulate genistein using a combined liquid–liquid phase separation method. The physicochemical properties of fabricated nanoparticles were characterized by dynamic light scattering (DLS), atomic force microscopy (AFM), and Fourier transform infrared spectroscopy (FTIR). The results demonstrated that genistein encapsulated with zein nanoparticles significantly improved its water dispersibility, antioxidant activity in the aqueous phase, and photostability against UV light. Moreover, genistein encapsulated in zein nanoparticles showed a sustained release property. Furthermore, it was found that encapsulation efficiency of genistein was significantly enhanced after CMCS coating, and this effect was more pronounced after the complex nanoparticles cross-linked with calcium ions when compared with the use of zein as a single encapsulant. In addition, compared to zein nanoparticles without biopolymer coating, CMCS coating significantly enhanced the thermal and storage stability of the formed nanoparticles, and delayed the release of genistein. A schematic diagram of zein and zein/carboxymethyl chitosan (CMCS) nanoparticles formation mechanism for encapsulation of genistein was proposed. According to the results of the current study, it could be concluded that encapsulation of genistein in zein/CMCS nanoparticles is a promising approach to improve its water dispersibility, antioxidant activity, photostability against UV light and provide controlled release for food/pharmaceutical applications.

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