Preparation and Characterization of Hydroxycamptothecin-Loaded Poly(D,L-lactic acid) Nanoparticles with High Drug Loading Capacity

2012 ◽  
Vol 531 ◽  
pp. 503-506
Author(s):  
Zhen Qing Hou ◽  
Shui Fan Zhou ◽  
Fei Cui ◽  
Yi Xiao Hang ◽  
Yun Feng Yi

Hydroxycamptothecin (HCPT) loaded PLA nanoparticles were prepared by a facile dialysis method. Three main influential factors, PLA concentration, ratio of HCPT to PLA (wt/wt), dialysis bags with different molecule weight cutoff, were evaluated using an orthogonal design, gave the nanoparticles with an average diameter of approximately 226.8 nm and fine drug loading content (5.16%, w/w). The in vitro drug release studies exhibited a slow and prolonged release profile over 30 days. It is concluded that the new method to prepare HCPT-PLA nanoparticles resulted in improved formulation characteristics including small size, high drug loading capacity, and long sustained drug release.

2017 ◽  
Vol 5 (21) ◽  
pp. 3898-3906 ◽  
Author(s):  
Yong-Gang Zhang ◽  
Ying-Jie Zhu ◽  
Feng Chen ◽  
Tuan-Wei Sun

The composite scaffold comprising ultralong hydroxyapatite microtubes and chitosan with high drug loading capacity and sustained drug release properties has been successfully prepared.


2020 ◽  
Vol 7 (4) ◽  
pp. 359-369
Author(s):  
Hai Zhang ◽  
Jianqin Yan ◽  
Heng Mei ◽  
Shengsheng Cai ◽  
Sai Li ◽  
...  

Abstract Challenges associated with low-drug-loading capacity, lack of active targeting of tumor cells and unspecific drug release of nanocarriers synchronously plague the success of cancer therapy. Herein, we constructed active-targeting, redox-activated polymeric micelles (HPGssML) self-assembled aptamer-decorated, amphiphilic biodegradable poly (benzyl malolactonate-co-ε-caprolactone) copolymer with disulfide linkage and π-conjugated moieties. HPGssML with a homogenous spherical shape and nanosized diameter (∼150 nm) formed a low critical micellar concentration (10−3 mg/mL), suggesting good stability of polymeric micelles. The anticancer drug, doxorubicin (DOX), can be efficiently loaded into the core of micelles with high-drug-loading content via strong π–π interaction, which was verified by a decrease in fluorescence intensity and redshift in UV adsorption of DOX in micelles. The redox sensitivity of polymeric micelles was confirmed by size change and in vitro drug release in a reducing environment. Confocal microscopy and flow cytometry assay demonstrated that conjugating aptamers could enhance specific uptake of HPGssML by cancer cells. An in vitro cytotoxicity study showed that the half-maximal inhibitory concentration (IC50) of DOX-loaded HPGssML was two times lower than that of the control group, demonstrating improved antitumor efficacy. Therefore, the multifunctional biodegradable polymeric micelles can be exploited as a desirable drug carrier for effective cancer treatment.


2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
Xin Leng ◽  
Hongliang Huang ◽  
Wenping Wang ◽  
Na Sai ◽  
Longtai You ◽  
...  

Drug delivery carriers with a high drug loading capacity and biocompatibility, especially for controlled drug release, are urgently needed due to the side effects and frequent dose in the traditional therapeutic method. Guided by nanomaterials, we have successfully synthesized zirconium-based metal−organic frameworks, Zr-TCPP (TCPP: tetrakis (4-carboxyphenyl) porphyrin), namely, PCN-222, which is synthesized by solvothermal method. And it has been designed as a drug delivery system (DDS) with a high drug loading of 38.77 wt%. In our work, PCN-222 has achieved pH-sensitive drug release and showed comprehensive SEM, TEM, PXRD, DSC, FTIR, and N2 adsorption-desorption. The low cytotoxicity and good biocompatibility of PCN-222 were certificated by the in vitro results from an MTT assay, DAPI staining, and Annexin V/PI double-staining even cultivated L02 cells and HepG2 cells for 48h. Furthermore, Oridonin, a commonly used cancer chemotherapy drug, is adsorbed into PCN-222 via the solvent diffusion technique. Based on an analysis of the Oridonin release profile, results suggest that it can last for more than 7 days in vitro. And cumulative release rate of Ori at the 7 d was about 86.29% and 63.23% in PBS (pH 5.5 and pH 7.2, respectively) at 37°C. HepG2 cells were chosen to research the cytotoxicity of PCN-222@Ori and free Oridonin. The results demonstrated that the PCN-222@Ori nanocarrier shows higher cytotoxicity in HepG2 cells compared to Oridonin.


2019 ◽  
Vol 7 (7) ◽  
pp. 1050-1055 ◽  
Author(s):  
Liangcan He ◽  
Kanglei Pang ◽  
Wenwen Liu ◽  
Yue Tian ◽  
Lin Chang ◽  
...  

Core–shell Au@zeolitic-imidazolate-framework nanocarriers with high drug-loading, controlled drug release properties, and high cancer treatment efficiency.


2019 ◽  
Vol 7 (28) ◽  
pp. 4402-4412 ◽  
Author(s):  
Mengwei Zou ◽  
Rongrong Jin ◽  
Yanfei Hu ◽  
Ying Zhang ◽  
Haibo Wang ◽  
...  

The thermo-sensitive hydrogels with high drug loading rate achieved sustained drug release over 2 weeks. Histopathological examination of retina confirmed the excellent biocompatibility and effective anti-inflammatory property of the hydrogel.


2017 ◽  
Vol 5 (12) ◽  
pp. 2501-2510 ◽  
Author(s):  
Zhaopei Guo ◽  
Xingzhi Zhou ◽  
Mengze Xu ◽  
Huayu Tian ◽  
Xuesi Chen ◽  
...  

Dimeric CPT (DCPT) could be largely encapsulated in polypeptide micelle RGD-PEG-g-PLL-b-PLeu (DRPPP) with redox-sensitive drug release capability, showing remarkable cellular uptakeviaRGD targeting, enhanced cytotoxicity and cell apoptosis.


2016 ◽  
Vol 52 (22) ◽  
pp. 4128-4131 ◽  
Author(s):  
Linyi Bai ◽  
Soo Zeng Fiona Phua ◽  
Wei Qi Lim ◽  
Avijit Jana ◽  
Zhong Luo ◽  
...  

Two nanoscale covalent organic frameworks as drug carriers with good biocompatibility were developed, showing high drug loading capacity and sustained release in vitro.


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