Parenteral nanosuspensions: a brief review from solubility enhancement to more novel and specific applications.
10.1016/j.apsb.2018.07.011
- Author:
Eknath AHIRE
1
;
Shreya THAKKAR
1
;
Mahesh DARSHANWAD
1
;
Manju MISRA
1
Author Information
1. Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad, Gujarat 380054, India.
- Publication Type:Journal Article
- Keywords:
ADME, absorption distribution metabolism elimination;
ASEs, aerosols solvent extractions;
AUC, area under curve;
BBB, blood–brain barrier;
BCS, Biopharmaceutical Classification System;
BDP, beclomethasone dipropionate;
CFC, critical flocculation concentration;
CLSM, confocal laser scanning microscopy;
CMC, critical micelle concentration;
DMSO, dimethyl sulfoxide;
EDI, estimated daily intake;
EHDA, electrohydrodynamic atomization;
EPAS, evaporative precipitation in aqueous solution;
EPR, enhanced permeability and retention;
FITC, fluorescein isothiocyanate;
GRAS, Generally Recognized as Safe;
HEC, hydroxyethylcellulose;
HFBII, class II hydrophobin;
HP-PTX/NC, hyaluronic acid-paclitaxel/nanocrystal;
HPC, hydroxypropyl cellulose;
HPH, high-pressure homogenization;
HPMC, hydroxypropyl methylcellulose;
IM, intramuscular;
IP, intraperitoneal;
IV, intravenous;
IVIVC, in vivo–in vitro correlation;
In vivo fate;
LD50, median lethal dose (50%);
MDR, multidrug resistance effect;
NCE, new chemical entities;
Nanosuspension;
P-gp, permeation glycoprotein;
PEG, polyethylene glycol;
PTX, paclitaxel;
PVA, polyvinyl alcohol;
Parenteral;
QbD, quality by design;
SC, subcutaneous;
SEDS, solution enhanced dispersion by supercritical fluids;
SEM, scanning electron microscopy;
SFL, spray freezing into liquids;
Scalability;
Solidification;
Stabilizer;
TBA, tert-butanol;
TEM, transmission electron microscopy;
US FDA, United States Food and Drug Administration;
Vitamin E TPGS, d-α-tocopheryl polyethylene glycol 1000 succinate
- From:
Acta Pharmaceutica Sinica B
2018;8(5):733-755
- CountryChina
- Language:English
-
Abstract:
Advancements in techniques of lead molecule selection have resulted in the failure of around 70% of new chemical entities (NCEs). Some of these molecules are getting rejected at final developmental stage resulting in wastage of money and resources. Unfavourable physicochemical properties affect ADME profile of any efficacious and potent molecule, which may ultimately lead to killing of NCE at final stage. Numerous techniques are being explored including nanocrystals for solubility enhancement purposes. Nanocrystals are the most successful and the ones which had a shorter gap between invention and subsequent commercialization of the first marketed product. Several nanocrystal-based products are commercially available and there is a paradigm shift in using approach from simply being solubility enhancement technique to more novel and specific applications. Some other aspects in relation to parenteral nanosuspensions are concentrations of surfactant to be used, scalability and fate. At present, there exists a wide gap due to poor understanding of these critical factors, which we have tried to address in this review. This review will focus on parenteral nanosuspensions, covering varied aspects especially stabilizers used, GRAS (Generally Recognized as Safe) status of stabilizers, scalability challenges, issues of physical and chemical stability, solidification techniques to combat stability problems and fate.
