Critical Reviews™ in Therapeutic Drug Carrier Systems, 36(1): 1–58 (2019)
0743-4863/19/$35.00 ©2019 Begell House, Inc. www.begellhouse.com 1
Polymeric Mixed Micelles: Improving the
Anticancer Effcacy of Single-Copolymer
Micelles
Arehalli S. Manjappa,
a,*
Popat S. Kumbhar,
a
Ajit B. Patil,
a
John I. Disouza,
a
&
Vandana B. Patravale
b
a
Tatyasaheb Kore College of Pharmacy, Warananagar, Tal: Panhala, Dist: Kolhapur,
Maharashtra, India;
b
Department of Pharmaceutical Sciences and Technology, Institute of Chemical
Technology, Nathalal Parekh Marg, Matunga, Mumbai, Maharashtra, India
*Address all correspondence to: Dr. Arehalli S. Manjappa, Assistant Professor, Department of Pharmaceutics,
Tatyasaheb Kore College of Pharmacy, Warananagar, Tal: Panhala, Dist: Kolhapur, Maharashtra, India, 416113;
Tel.: (02328) 223526; Fax: (02328) 223501, E-mail: manju_as82@yahoo.co.in
ABSTRACT: Mixed micelles self-assembled from two or more dissimilar block copolymers
provide a direct and convenient approach to improved drug delivery. The present review is
focused on mixed micelles (prepared from block copolymers only) for various drug delivery
applications along with their merits over single-copolymer micelles. Presented are the physi-
cochemical properties of mixed and single-copolymer micelles, various stimuli-responsive
mixed micelles for the treatment of cancer, interesting combinations of multifunctional mixed
micelles along with their in vitro and in vivo performance, and the potential of mixed micelles
as a gene delivery system. Finally, the performance of mixed micelles in preclinical and clini-
cal testing is explained. In addition, the interaction of mixed micelles with cancer cells and the
biosafety of mixed micelles are summarized. The in vitro and in vivo performance presented
here clearly reveals that the mixed-micelle approach has a wider scope than that of the single-
copolymer micelle approach and directs researchers to focus on this approach to delivery of
drugs/gene/biologics for various applications.
KEY WORDS: mixed micelles, single-copolymer micelles, block copolymers, drug delivery,
gene delivery
ABBREVIATIONS: 17-AAG, 17-allyamino-17-demethoxygeldanamycin; apoB, apolipoprotein B; AUC,
area under the curve; BDMC, bisdemethoxy curcumin; BHS-I, baohuoside I; BPD, benzoporphyrin deriva-
tives; BPDMA, benzoporphyrin derivative monoacid A-ring; BPDMB, benzoporphyrin derivative mono-
acid B-ring; BSA, bovine serum albumin; CMC, critical micelle concentration; CPT, camptothecin; CUR,
curcumin; DIR, 1,1′-dDioctadecyl-3,3,3′,3′-tetramethylindotricarbocyanine; DLC, drug-loading capacity;
DNA, deoxyribonucleic acid; DOX, doxorubicin; DTT, dithiothreitol; DTX, docetaxel; EE, entrapment
efciency; EFV, efavirenz; FDA, Food And Drug Administration; FPF, Pluronic P123/F127 mixed mi-
celles decorated with folic acid; GAG, glycosaminoglycan; GalNAc, N-acetylgalactosamine; GEJ, gas-
troesophageal junction; GI tract, gastrointestinal tract; Glu, glucosamine; GSH, glutathione; i.v., intrave-
nous; IC
50
, median inhibition concentration; ITT, intent-to-treat; JGN, juglon; MDR, multidrug resistant;
MMs, mixed micelles; MPMs, mixed polyplex micelles; MPS, mean particle size; MRT, mean residential
time; MTX, methotrexate; MYR, myricetin; NCL, niclosamide NiPAAM, N-isopropylacrylamide; ORN,
oridonin; PAT, parthenolide; PBS, phosphate bufer saline; PDI, polydispersity index; PDMAEMA,
poly((dimethylamino)ethylene methacrylate); pDNA, plasmid DNA; PDPA, poly(2 (diisopropylamino)eth-