Abstract
Nanocrystalline materials (NCM, i.e., crystalline nanoparticles) have become an important class of materials with great potential for applications ranging from drug delivery and electronics to optics. Drug nanocrystals (NC) and nano co-crystals (NCC) are examples of NCM with fascinating physicochemical properties and have attracted significant attention in drug delivery. NCM are categorized by advantageous properties, such as high drug-loading efficiency, good long-term physical stability, steady and predictable drug release, and long systemic circulation time. These properties make them excellent formulations for the efficient delivery of a variety of active pharmaceutical ingredients (API). In this review, we summarize the recent advances in drug NCM-based therapy options. Currently, there are three main methods to synthesize drug NCM, including top-down, bottom-up, and combination methods. The fundamental characterization methods of drug NCM are elaborated. Furthermore, the applications of these characterizations and their implications on the post-formulation performance of NCM are introduced.
Highlights
There has been an increasing interest in developing drug delivery systems that circumvent the challenges associated with conventional drug delivery [1]
We focus on the characterization of organic NCM for the delivery of active pharmaceutical ingredients (API)
The high-pressure homogenization (HPH) method occurs via the following steps: of (i) crude API powder is dispersed in pure solution or in a solution containing a stabiliser, (ii) a reduction of particle size occurs by high-speed shearing or homogenization under low pressure, (iii) HPH is used to achieve the target particle size and size distribution
Summary
There has been an increasing interest in developing drug delivery systems that circumvent the challenges associated with conventional drug delivery [1]. This was Crystals 2021, 11, 310 explored and showed favourable outcomes when utilized in formulations containing budesonide, dexamethasone, hydrocortisone, prednisolone [31], and fluorometholone [31,32]. Targeted delivery approaches have been implemented in combination with NC and NCC technology for drugs that exhibit low bioavailability, poor aqueous solubility and stability, and limited in vitro–in vivo correlations (IVIVC) [39,40]. Surface modification of lamivudine-zidovudine NCC with sodium dodecyl sulphate (SDS) and α-tocopheryl polyethylene glycol succinate 1000 (TPGS 1000) was reported to have reduced cytotoxic effect on HeLa cells [42] Despite their success in drug delivery, NCM have to undergo rigorous characterization prior to their use in humans. Formulation and morphology of drug NCM, including fundamental characterizations and their implications on post-formulation performance are described below
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