Emerging role of nanosuspensions in drug delivery systems

Abstract

Rapid advancement in drug discovery process is leading to a number of potential new drug candidates having excellent drug efficacy but limited aqueous solubility. By virtue of the submicron particle size and distinct physicochemical properties, nanosuspension has the potential ability to tackle many formulation and drug delivery issues typically associated with poorly water and lipid soluble drugs. Conventional size reduction equipment such as media mill and high-pressure homogenizers and formulation approaches such as precipitation, emulsion-solvent evaporation, solvent diffusion and microemulsion techniques can be successfully implemented to prepare and scale-up nanosuspensions. Maintaining the stability in solution as well as in solid state, resuspendability without aggregation are the key factors to be considered for the successful production and scale-up of nanosuspensions. Due to the considerable enhancement of bioavailability, adaptability for surface modification and mucoadhesion for drug targeting have significantly expanded the scope of this novel formulation strategy. The application of nanosuspensions in different drug delivery systems such as oral, ocular, brain, topical, buccal, nasal and transdermal routes are currently undergoing extensive research. Oral drug delivery of nanosuspension with receptor mediated endocytosis has the promising ability to resolve most permeability limited absorption and hepatic first-pass metabolism related issues adversely affecting bioavailability. Advancement of enabling technologies such as nanosuspension can solve many formulation challenges currently faced among protein and peptide-based pharmaceuticals.

Quality by Design (QbD) Approach for Optimization and Characterization of Micro emulsion based Nasal formulation of Antipsychotic/Antischizophrenic Drug-Aripiprazole

“…Aripiprazole is atypical antipsychotic drug, exhibits very low aqueous solubility and high lipophilicity and thus classified as BCS Class IV drug. [1][2][3][4] In present investigation, this poorly water soluble drug Aripiprazole is successful incorporated into micro-emulsion by Qbd approach. Based on solubility, oleic acid is selected as oil phase while Tween 80 and Transcutol -p are selected as surfactants and co surfactants respectively for micro-emulsion formulation.…”

“…3 4 factorial design based on Box Behnken Experimental design for response surface Methodology was applied for optimization of formulation variables. Oleic acid(X1), Tween 80(X2), Transcutol-p(X3) and Water (X4) were taken as independent variables while Particle size (Y1) and Drug content (Y2) were taken as dependent variables to study 3D response plots [ Figure 2].…”

“…3 Micro emulsion technique offers a promising solution for solubilisation of such drugs during formulation. 4 Intranasal route is one of the advanced approaches to deliver antipsychotic or neuroprotective drug directly to brain via olfactory and trigeminal nerves through cavity by avoiding blood brain barrier hurdle. 5 QBD is now an integral part of formulation development at lab as well as industrial level because factorial design gives best optimized batch for pilot plant scale up.…”

Preparation of high drug-loading celastrol nanosuspensions and their anti-breast cancer activities in vitro and in vivo

“…In the past two decades, with the widespread application of high-throughput screening and combinatorial chemistry in drug discovery, many antitumor active compounds have been discovered, but most of that have shown poor aqueous solubility. This poor solubility is a major challenge for formulation of these compounds for both oral and intravenous administration 1,2 .…”

“…Nanosuspensions are sub-micron colloidal dispersions composed of an almost pure drug core stabilized by a small amount of surfactants or amphipathic block-copolymers 22,23 . Therefore, nanosuspensions are characteristic of very high drug loading content, which reaches up to 100%.…”