High drug-loading nanomedicines: progress, current status, and prospects

Abstract

Drug molecules transformed into nanoparticles or endowed with nanostructures with or without the aid of carrier materials are referred to as “nanomedicines” and can overcome some inherent drawbacks of free drugs, such as poor water solubility, high drug dosage, and short drug half-life in vivo. However, most of the existing nanomedicines possess the drawback of low drug-loading (generally less than 10%) associated with more carrier materials. For intravenous administration, the extensive use of carrier materials might cause systemic toxicity and impose an extra burden of degradation, metabolism, and excretion of the materials for patients. Therefore, on the premise of guaranteeing therapeutic effect and function, reducing or avoiding the use of carrier materials is a promising alternative approach to solve these problems. Recently, high drug-loading nanomedicines, which have a drug-loading content higher than 10%, are attracting increasing interest. According to the fabrication strategies of nanomedicines, high drug-loading nanomedicines are divided into four main classes: nanomedicines with inert porous material as carrier, nanomedicines with drug as part of carrier, carrier-free nanomedicines, and nanomedicines following niche and complex strategies. To date, most of the existing high drug-loading nanomedicines belong to the first class, and few research studies have focused on other classes. In this review, we investigate the research status of high drug-loading nanomedicines and discuss the features of their fabrication strategies and optimum proposal in detail. We also point out deficiencies and developing direction of high drug-loading nanomedicines. We envision that high drug-loading nanomedicines will occupy an important position in the field of drug-delivery systems, and hope that novel perspectives will be proposed for the development of high drug-loading nanomedicines.

Taxanes Hybrid Nanovectors: From Design to Physico‐Chemical Evaluation of Docetaxel and Paclitaxel Gold (III)‐PEGylated Complex Nanocarriers

“…In order to better understand the intrinsic differences between these two nanomedicine candidates, comparative Raman studies were carried out at pH 7.0 and 4.0 in order to follow the PTX and DTX release under a range time(from 1 to 96 h) (Figures S1A and S2A, Supporting Information). Previously, other authors have demonstrated spectroscopical differences and variation of chemical conformation during drug release profiles . Thus, PTX IN‐PEG‐AuNPs and DTX IN‐PEG‐AuNPs were characterized by Raman spectroscopy after incubation for 96 h in PBS at 37 °C in order to (1) confirm the drug release and (2) to evaluate variations in the chemical orientation of PTX and DTX at pH 4.0 (when PTX and DTX are protonated) and pH 7.0 (when PTX and DTX are partially deprotonated).…”

“…It was demonstrated that effective DOX release was carried out at pH 4, with stability attained at AuNP diameter close to 20 nm in physiological pH. This strategy can be applied to any drugs possessing complexation ability, such as carboxylates, phosphonates, including anthracycline, alkaloid, and flavonoid . The particle size and pH‐responsive point of nano‐therapeutics are dependent on the complex combinations of polymer ligands, drug molecules, and center metal ions .…”

“…This strategy can be applied to any drugs possessing complexation ability, such as carboxylates, phosphonates, including anthracycline, alkaloid, and flavonoid . The particle size and pH‐responsive point of nano‐therapeutics are dependent on the complex combinations of polymer ligands, drug molecules, and center metal ions . The purpose of this study is to provide novel nanomedicines for biological applications by using taxanes (DTX or PTX) complexed to gold ions to build nanoparticles (DTX IN PEG‐AuNPs; PTX‐IN PEG‐AuNPs), with different chemical‐physical properties to improve their biological activity.…”

Kinetics of drug release profile from maleic anhydride-grafted-chitosan film

“…In the application of the drug delivery system, one of the important properties of the system is a large capacity of the drug loading [6]. One effort that can be done to improve the properties is modification through the crosslinking method.…”

Current Advances of Hollow Capsules as Controlled Drug Delivery Systems

“…The utilization of controlled drug delivery systems provides a great number of advantages compared to those of traditional drug‐dosage forms, for instance, enhanced efficiency and stability, diminished toxicity, reduced side effects and capability to administrate the delivery of drugs to the active site . Biocompatibility, biodegradability, low cytotoxicity, high drug‐loading capacity and ease to monitor pharmacokinetic release profiles are the most desirable features of an ideal drug delivery system …”