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.

scholarly journals Considerable Improvement of Ursolic Acid Water Solubility by Its Encapsulation in Dendrimer Nanoparticles: Design, Synthesis and Physicochemical Characterization

Nanomaterials ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 2196 ◽  
Author(s):  
Silvana Alfei ◽  
Anna Maria Schito ◽  
Guendalina Zuccari
Keyword(s):  
Ursolic Acid ◽  
Water Solubility ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Systemic Toxicity ◽  
Water Soluble ◽  
Design Synthesis ◽  
Pentacyclic Triterpenoid

Ursolic acid (UA) is a pentacyclic triterpenoid found in many medicinal plants and aromas endowed with numerous in vitro pharmacological activities, including antibacterial effects. Unfortunately, UA is poorly administered in vivo, due to its water insolubility, low bioavailability, and residual systemic toxicity, thus making urgent the development of water-soluble UA formulations. Dendrimers are nonpareil macromolecules possessing highly controlled size, shape, and architecture. In dendrimers with cationic surface, the contemporary presence of inner cavities and of hydrophilic peripheral functions, allows to encapsulate hydrophobic non-water-soluble drugs as UA, to enhance their water-solubility and stability, and to promote their protracted release, thus decreasing their systemic toxicity. In this paper, aiming at developing a new UA-based antibacterial agent administrable in vivo, we reported the physical entrapment of UA in a biodegradable not cytotoxic cationic dendrimer (G4K). UA-loaded dendrimer nanoparticles (UA-G4K) were obtained, which showed a drug loading (DL%) much higher than those previously reported, a protracted release profile governed by diffusion mechanisms, and no cytotoxicity. Also, UA-G4K was characterized by principal components analysis (PCA)-processed FTIR spectroscopy, by NMR and elemental analyses, and by dynamic light scattering experiments (DLS). The water solubility of UA-G4K was found to be 1868-fold times higher than that of pristine UA, thus making its clinical application feasible.

Importance of Encapsulation Stability of Nanocarriers with High Drug Loading Capacity for Increasing in Vivo Therapeutic Efficacy

2018 ◽  
Vol 19 (7) ◽  
pp. 3030-3039 ◽  
Author(s):  
L. Palanikumar ◽  
Eun Seong Choi ◽  
Jun Yong Oh ◽  
Soo Ah Park ◽  
Huyeon Choi ◽  
...  
Keyword(s):  
Therapeutic Efficacy ◽  
Drug Loading ◽  
Loading Capacity ◽  
High Drug ◽  
High Drug Loading

Investigating the influence of aromatic moieties on the formulation of hydrophobic natural products and drugs in poly(2-oxazoline) based amphiphiles

2018 ◽  
Author(s):  
Robert Luxenhofer ◽  
Michael M Lübtow ◽  
Lukas Hahn ◽  
Thomas Lorson ◽  
Rainer Schobert
Keyword(s):  
Natural Products ◽  
Small Molecules ◽  
Water Solubility ◽  
Drug Loading ◽  
High Drug ◽  
Long Term Stability ◽  
Aromatic Content ◽  
Important Interaction ◽  
Amorphous Structures ◽  
High Drug Loading

Many natural compounds with interesting biomedical properties share one physicochemical property, namely a low water solubility. Polymer micelles are, among others, a popular means to solubilize hydrophobic compounds. The specific molecular interactions between the polymers and the hydrophobic drugs are diverse and recently it has been discussed that macromolecular engineering can be used to optimize drug loaded micelles. Specifically, π-π stacking between small molecules and polymers has been discussed as an important interaction that can be employed to increase drug loading and formulation stability. Here, we test this hypothesis using four different polymer amphiphiles with varying aromatic content and various natural products that also contain different relative amounts of aromatic moieties. While in the case of paclitaxel, having the lowest relative content of aromatic moieties, the drug loading decreases with increasing relative aromatic amount in the polymer, the drug loading of curcumin, having a much higher relative aromatic content, is increased. Interestingly, the loading using schizandrin A, a dibenzo[a,c]cyclooctadiene lignan with intermediate relative aromatic content is not influenced significantly by the aromatic content of the polymers employed. The very high drug loading, long term stability, the ability to form stable highly loaded binary coformulations in different drug combinations, small sized formulations and amorphous structures in all cases, corroborate earlier reports that poly(2-oxazoline) based micelles exhibit an extraordinarily high drug loading and are promising candidates for further biomedical applications. The presented results underline that the interaction between the polymers and the incorporated small molecules are complex and must be investigated in every specific case.<br>

Design of dual-responsive nanocarries with high drug loading capacity based on hollow mesoporous organosilica nanoparticles

2019 ◽  
Vol 233 ◽  
pp. 230-235 ◽  
Author(s):  
Li-li Lu ◽  
Wen-ya Xiong ◽  
Jun-bin Ma ◽  
Tian-fang Gao ◽  
Si-yuan Peng ◽  
...  
Keyword(s):  
Drug Loading ◽  
Loading Capacity ◽  
High Drug ◽  
Dual Responsive ◽  
Mesoporous Organosilica ◽  
High Drug Loading

scholarly journals Cancer Nanomedicines Stabilized by π-π Stacking between Heterodimeric Prodrugs Enable Exceptionally High Drug Loading Capacity and Safer Delivery of Drug Combinations

Theranostics ◽  
2017 ◽  
Vol 7 (15) ◽  
pp. 3638-3652 ◽  
Author(s):  
Hangxiang Wang ◽  
Jianmei Chen ◽  
Chang Xu ◽  
Linlin Shi ◽  
Munire Tayier ◽  
...  
Keyword(s):  
Drug Loading ◽  
Drug Combinations ◽  
Loading Capacity ◽  
High Drug ◽  
Π Stacking ◽  
High Drug Loading

A γ-cyclodextrin-based metal–organic framework embedded with graphene quantum dots and modified with PEGMA via SI-ATRP for anticancer drug delivery and therapy

Nanoscale ◽  
2019 ◽  
Vol 11 (43) ◽  
pp. 20956-20967 ◽  
Author(s):  
Qiaojuan Jia ◽  
Zhenzhen Li ◽  
Chuanpan Guo ◽  
Xiaoyu Huang ◽  
Yingpan Song ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Metal Organic Framework ◽  
Drug Loading ◽  
Graphene Quantum Dots ◽  
Tumor Growth Inhibition ◽  
High Drug ◽  
Anticancer Drug Delivery ◽  
Metal Organic ◽  
High Drug Loading

A biocompatible γ-CD-MOF based DDS with high drug loading and full drug release was prepared and effective tumor growth inhibition was achieved in vivo.

scholarly journals Synthesis and compatibility evaluation of versatile mesoporous silica nanoparticles with red blood cells: an overview

RSC Advances ◽  
2019 ◽  
Vol 9 (61) ◽  
pp. 35566-35578 ◽  
Author(s):  
Subhankar Mukhopadhyay ◽  
Hanitrarimalala Veroniaina ◽  
Tadious Chimombe ◽  
Lidong Han ◽  
Wu Zhenghong ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Blood Cells ◽  
Drug Delivery Systems ◽  
Mesoporous Silica Nanoparticles ◽  
Drug Loading ◽  
Loading Capacity ◽  
High Drug ◽  
High Drug Loading

Protean mesoporous silica nanoparticles are propitious candidates over decades for nanoscale drug delivery systems due to their unique characteristics, including changeable pore size, mesoporosity, high drug loading capacity and biodegradability.

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