A Novel Preparation Method for Octreotide Acetate-Loaded PLGA Microspheres with a High Drug-Loading Capacity and a Low Initial Burst Release, and Its Studies on Relations between In Vitro and In Vivo Release

2013 ◽  
Vol 32 (3) ◽  
pp. n/a-n/a
Author(s):  
Bin Chen ◽  
Bing Han ◽  
Liping Song ◽  
Dan Xu ◽  
Jin Pei
Keyword(s):  
Preparation Method ◽  
Drug Loading ◽  
Burst Release ◽  
Loading Capacity ◽  
Plga Microspheres ◽  
High Drug ◽  
In Vivo Release ◽  
High Drug Loading

Water soluble multiarm-polyethylene glycol–betulinic acid prodrugs: design, synthesis, and in vivo effectiveness

2014 ◽  
Vol 5 (19) ◽  
pp. 5775-5783 ◽  
Author(s):  
Lin Dai ◽  
Dan Li ◽  
Jing Cheng ◽  
Jing Liu ◽  
Li-Hong Deng ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Betulinic Acid ◽  
Water Solubility ◽  
Drug Loading ◽  
Water Soluble ◽  
Loading Capacity ◽  
Design Synthesis ◽  
High Drug ◽  
High Drug Loading

Multiarm-polyethylene glycol–betulinic acid prodrugs were prepared by using multiarm-polyethylene glycol linkers and betulinic acid, which exhibited high drug loading capacity, good water solubility, and excellent anticancer activity.

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
Keyword(s):  
Drug Release ◽  
Orthogonal Design ◽  
Drug Loading ◽  
Influential Factors ◽  
Prolonged Release ◽  
Loading Capacity ◽  
Sustained Drug Release ◽  
High Drug ◽  
High Drug Loading

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.

scholarly journals High-drug-loading capacity of redox-activated biodegradable nanoplatform for active targeted delivery of chemotherapeutic drugs

2020 ◽  
Vol 7 (4) ◽  
pp. 359-369
Author(s):  
Hai Zhang ◽  
Jianqin Yan ◽  
Heng Mei ◽  
Shengsheng Cai ◽  
Sai Li ◽  
...  
Keyword(s):  
Drug Release ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Active Targeting ◽  
Control Group ◽  
Loading Capacity ◽  
Disulfide Linkage ◽  
High Drug ◽  
High Drug Loading

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.

Nanoscale covalent organic frameworks as smart carriers for drug delivery

2016 ◽  
Vol 52 (22) ◽  
pp. 4128-4131 ◽  
Author(s):  
Linyi Bai ◽  
Soo Zeng Fiona Phua ◽  
Wei Qi Lim ◽  
Avijit Jana ◽  
Zhong Luo ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Drug Loading ◽  
Drug Carriers ◽  
Loading Capacity ◽  
Covalent Organic Frameworks ◽  
High Drug ◽  
Good Biocompatibility ◽  
High Drug Loading

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

scholarly journals A novel preparative method for nanoparticle albumin-bound paclitaxel with high drug loading and its evaluation both in vitro and in vivo

PLoS ONE ◽  
2021 ◽  
Vol 16 (4) ◽  
pp. e0250670
Author(s):  
Yue Gao ◽  
Jingxue Nai ◽  
Zhenbo Yang ◽  
Jinbang Zhang ◽  
Siyu Ma ◽  
...  
Keyword(s):  
Self Assembly ◽  
Drug Loading ◽  
Preparative Method ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Spectra Analysis ◽  
High Drug ◽  
High Drug Loading

We developed a novel preparative method for nanoparticle albumin-bound (nab) paclitaxel with high drug loading, which was based on improved paclitaxel solubility in polyethylene glycol (PEG) and self-assembly of paclitaxel in PEG with albumin powders into nanoparticles. That is, paclitaxel and PEG were firstly dissolved in ethanol, which was subsequently evaporated under vacuum. The obtained liquid was then mixed with human serum albumin powders. Thereafter, the mixtures were added into phosphate-buffered saline and nab paclitaxel suspensions emerged after ultrasound. Nab paclitaxel was finally acquired after dialysis and freeze drying. The drug loading of about 15% (W/V) were realized in self-made nab paclitaxel, which was increased by approximately 50% compared to 10% (W/V) in Abraxane. Now this new preparative method has been authorized to obtain patent from China and Japan. The similar characteristics of self-made nab paclitaxel compared to Abraxane were observed in morphology, encapsulation efficiency, in vitro release, X-ray diffraction analysis, differential scanning calorimetry analysis, and circular dichroism spectra analysis. Consistent concentration-time curves in rats, biodistributions in mice, anti-tumor activities in mice, and histological transmutation in mice were also found between Abraxane and self-made nanoparticles. In a word, our novel preparative method for nab paclitaxel can significantly improve drug loading, obviously decrease product cost, and is considered to have potent practical value.

scholarly journals Efficient Self-Assembly of mPEG End-Capped Porous Silica as a Redox-Sensitive Nanocarrier for Controlled Doxorubicin Delivery

2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
Anh Khoa Nguyen ◽  
Thi Hiep Nguyen ◽  
Bui Quoc Bao ◽  
Long Giang Bach ◽  
Dai Hai Nguyen
Keyword(s):  
Self Assembly ◽  
Drug Loading ◽  
Porous Silica ◽  
Average Diameter ◽  
Burst Release ◽  
Loading Capacity ◽  
Potential Candidate ◽  
High Drug ◽  
Poly Ethylene ◽  
High Drug Loading

Porous nanosilica (PNS) has been regarded as a promising candidate for controlled delivery of anticancer drugs. Unmodified PNS-based nanocarriers, however, showed a burst release of encapsulated drugs, which may limit their clinical uses. In this report, PNS was surface conjugated with adamantylamine (ADA) via disulfide bridges (-SS-), PNS-SS-ADA, which was further modified with cyclodextrin-poly(ethylene glycol) methyl ether conjugate (CD-mPEG) to form a core@shell structure PNS-SS-ADA@CD-mPEG for redox triggered delivery of doxorubicin (DOX), DOX/PNS-SS-ADA@CD-mPEG. The prepared PNS-SS-ADA@CD-mPEG nanoparticles were spherical in shape with an average diameter of 55.5 ± 3.05 nm, a little larger than their parentally PNS nanocarriers, at 49.6 ± 2.56 nm. In addition, these nanoparticles possessed high drug loading capacity, at 79.2 ± 3.2%, for controlled release. The release of DOX from DOX/PNS-SS-ADA@CD-mPEG nanoparticles was controlled and prolonged up to 120 h in PBS medium (pH 7.4), compared to less than 40 h under reducing condition of 5 mM DTT. Notably, the PNS-SS-ADA@CD-mPEG was a biocompatible nanocarrier, and the toxicity of DOX was dramatically reduced after loading drugs into the porous core. This redox-sensitive PNS-SS-ADA@CD-mPEG nanoparticle could be considered a potential candidate with high drug loading capacity and a lower risk of systemic toxicity.

scholarly journals Intravenous delivery of enzalutamide based on high drug loading multifunctional graphene oxide nanoparticles for castration-resistant prostate cancer therapy

2020 ◽  
Author(s):  
Wenjun Jiang ◽  
Jiyuan Chen ◽  
Chunai Gong ◽  
Yuanyuan Wang ◽  
Yuan Gao ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Graphene Oxide ◽  
Drug Loading ◽  
Electron Interaction ◽  
Castration Resistant Prostate Cancer ◽  
High Drug ◽  
Castration Resistant ◽  
High Drug Loading

Abstract Background: Enzalutamide (Enz) has shown limited bioavailability via oral administration. It is easy for patients to develop into castration-resistant prostate cancer (CRPC) due to resistance to 18-24 months of androgen deprivation therapy (ADT). Moreover, it is hard to delivery Enz in vivo for low drug loading (DL) and encapsulation efficiency (EE).Therefore, we developed a multifunctional enzalutamide-loaded graphene oxide nanosystem (TP-GQDss/Enz) for castration-resistant prostate cancer (CRPC) intravenous treatment, with high drug loading efficiency.Methods: Aminated graphene quantum dots (GQDs) were first cross-linked via disulfide bonds into a graphene quantum dot derivative of approximately 200 nm (GQDss), which was further functionalized with a tumour-targeting peptide and PEG to form TP-GQDss. Enz was loaded into TP-GQDss for in vitro and in vivo study.Results: The results showed that high drug-loading efficiency was achieved by TP-GQDss via π-π electron interaction. TP-GQDss could be rapidly internalized by CRPC cells via endocytosis. Moreover, Enz in TP-GQDss could promote the inhibition of cell growth in vitro against CRPC cells. Further, TP-GQDss exhibited an enhanced cancer-targeting ability and alleviated the side effects of Enz in vivo. Conclusions: The multifunctional nanocarrier constructed here could accomplish controlled Enz release and serve as an intravenous therapy platform for CRPC.

scholarly journals Intravenous delivery of enzalutamide based on high drug loading multifunctional graphene oxide nanoparticles for castration-resistant prostate cancer therapy

2019 ◽  
Author(s):  
Wenjun Jiang ◽  
Jiyuan Chen ◽  
Chunai Gong ◽  
Yuanyuan Wang ◽  
Yuan Gao ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Graphene Oxide ◽  
Drug Loading ◽  
Castration Resistant Prostate Cancer ◽  
High Drug ◽  
Castration Resistant ◽  
Drug Loading Efficiency ◽  
High Drug Loading

Abstract Background: Enzalutamide (Enz) has shown limited bioavailability via oral administration and is easy for patients to develop into castration-resistant prostate cancer (CRPC) due to resistance to 18-24 months of androgen deprivation therapy (ADT). Moreover, it is hard to delivery Enz for low drug loading (DL) and encapsulation efficiency (EE). Therefore, we developed a multifunctional enzalutamide-loaded graphene oxide nanosystem (TP-GQDss/Enz) for castration-resistant prostate cancer (CRPC) intravenous treatment, with high drug loading efficiency and good biocompatibility.Methods: Aminated graphene quantum dots (GQDs) were first cross-linked via a disulfide bond into a graphene quantum dot derivative of approximately 200 nm (GQDss), which was further functionalized with a tumour-targeting peptide and PEG to form TP-GQDss. Enz was loaded into TP-GQDss for in vitro and in vivo study.Results: The results showed that high drug-loading efficiency was achieved by TP-GQDss via π-π electron interaction. TP-GQDss could be rapidly internalized by CRPC cells via endocytosis. Moreover, Enz in TP-GQDss could promote the inhibition of cell growth in vitro against CRPC cells, while TP-GQDss alone did not show any obvious cytotoxicity on CRPC cells after 24 h of incubation. Further, TP-GQDss exhibited an enhanced cancer-targeting ability and alleviated the side effects of Enz in vivo. Conclusions: The multifunctional nanocarrier constructed here could accomplish controlled Enz release and serve as a intravenous therapy platform for CRPC.

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