Introduction:
1.1 Rationale of developing drug nanosuspension
One of the primary goals of drug research in recent decades has been to increase the
bioavailability of medications that are poorly soluble in water. the solubility and rate of
dissolution of poorly water-soluble Biopharmaceutics Classification System (BCS) Class II & IV
medications limit their bioavailability.
Poor water solubility affects over 40% of the active pharmaceutical ingredients (API) that are
now being used in industry pipelines. Thus, formulations with higher rates of dissolution are
desperately needed in the industry to improve absorption and bioavailability (Dalvi et al., 2012).
There is little use for traditional methods that were developed earlier to address the formulation
issues, such as micronization, solubilization with co-solvents, the use of permeation enhancers
(Aungst et al., 1993 & 2000), oily solutions (Aungst et al., 1993), and surfactant dispersions
(Aungst et al., 1994).
Furthermore, the majority of these methods need a lot of chemicals, which restricts their
application from a safety standpoint. therefore, a novel approach that may address formulation-
related issues related to hydrophobic drug delivery is becoming increasingly necessary to
enhance clinical efficacy and maximize therapy in terms of pharmacoeconomics.
Because of their simplicity and the benefits they offer over alternative approaches,
nanosuspensions have shown promise in addressing the issues related to the delivery of poorly
water-soluble and poorly water- and lipid-soluble medications.
1.1.1 Nanosuspensions
According to Chingunpituk et al. (2007), nanosuspension is a sub-micron colloidal dispersion of
medicine particles stabilized by polymers, surfactants, or a combination of the two.
According to Date et al. (2004), this formulation is inexpensive, has a high drug loading, and a
low frequency of excipient-induced adverse effects.
According to Kayser et al. (2003), nanoparticles have the ability to stick to the gastrointestinal
mucosa, extending the drug’s contact duration and improving absorption.
One benefit of nanosuspensions is that they can be administered by a variety of routes, including
oral (Kesisoglou et al., 2007), parenteral (Xiong et al., 2008 & Wong, 2008), pulmonary (Jacobs
et al., 2002), dermal (Mishra et al., 2009), and ocular (Kassem et al., 2007).