Strategies for improving the payload of small molecular drugs in polymeric micelles.
In the past few years, substantial efforts have been made in the design and preparation of polymeric micelles as novel drug delivery vehicles. Typically, polymeric micelles possess a spherical core-shell structure, with a hydrophobic core and a hydrophilic shell. Consequently, poorly water-soluble drugs can be effectively solubilized within the hydrophobic core, which can significantly boost their drug loading in aqueous media. This leads to new opportunities for some bioactive compounds that have previously been abandoned due to their low aqueous solubility. Even so, the payload of small molecular drugs is still not often satisfactory due to low drug loading and premature release, which makes it difficult to meet the requirements of in vivo studies. This problem has been a major focus in recent years. Following an analysis of the published literature in this field, several strategies towards achieving polymeric micelles with high drug loading and stability are presented in this review, in order to ensure adequate drug levels reach target sites.
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China; Jiangsu Kanion Pharmaceutical Co., Ltd., Lianyungang 222047, China. Electronic address: pharmzy@163.com.
Yu
Y
Zhang
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China.
Tianyang
T
Ren
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China.
Jingxin
J
Gou
Department of Biotherapy, Cancer Research Institute, The First Affiliated Hospital of China Medical University, Shenyang 110001, China.
Ling
L
Zhang
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China.
Xiaoguang
X
Tao
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China.
Bin
B
Tian
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China.
Pengqian
P
Tian
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China.
Dandan
D
Yu
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China.
Jianbo
J
Song
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China.
Xiaolin
X
Liu
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China.
Yanhui
Y
Chao
Jiangsu Kanion Pharmaceutical Co., Ltd., Lianyungang 222047, China.
Wei
W
Xiao
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China. Electronic address: tanglab@126.com.
Xing
X
Tang
D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D065546:Drug Liberation; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008823:Micelles; D004364:Pharmaceutical Preparations / Q000008:administration & dosage / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D012995:Solubility
D004337:Drug Carriers; D008823:Micelles; D004364:Pharmaceutical Preparations; D011108:Polymers
10-Hydroxycamptothecin (PubChem CID: 97226); Amphotericin B (PubChem CID:5280965); Capecitabine (PubChem CID: 60953); Cisplatin (PubChem CID: 2767); Coenzyme Q10 (PubChem CID: 5281915); Docetaxel (PubChem CID: 148124); Doxorubicin (PubChem CID: 31703); Drug loading; Paclitaxel (PubChem CID: 36314); Payload; Polymeric micelles; Premature release; Small molecular drugs