Novel Nanostructured Solid Materials for Modulating Oral Drug Delivery from Solid-State Lipid-Based Drug Delivery Systems

Abstract

Lipid-based drug delivery systems (LBDDS) have gained significant attention in recent times, owing to their ability to overcome the challenges limiting the oral delivery of poorly water-soluble drugs. Despite the successful commercialization of several LBDDS products over the years, a large discrepancy exists between the number of poorly water-soluble drugs displaying suboptimal in vivo performances and the application of LBDDS to mitigate their various delivery challenges. Conventional LBDDS, including lipid solutions and suspensions, emulsions, and self-emulsifying formulations, suffer from various drawbacks limiting their widespread use and commercialization. Accordingly, solid-state LBDDS, fabricated by adsorbing LBDDS onto a chemically inert solid carrier material, have attracted substantial interest as a viable means of stabilizing LBDDS whilst eliminating some of the various limitations. This review describes the impact of solid carrier choice on LBDDS performance and highlights the importance of appropriate solid carrier material selection when designing hybrid solid-state LBDDS. Specifically, emphasis is placed on discussing the ability of the specific solid carrier to modulate drug release, control lipase action and lipid digestion, and enhance biopharmaceutical performance above the original liquid-state LBDDS. To encourage the interested reader to consider their solid carrier choice on a higher level, various novel materials with the potential for future use as solid carriers for LBDDS are described. This review is highly significant in guiding future research directions in the solid-state LBDDS field and fostering the translation of these delivery systems to the pharmaceutical marketplace.

Modulating the Lipase‐Mediated Bioactivity of Particle‐Lipid Conjugates Through Changes in Nanostructure and Surface Chemistry

“…The large clay platelets aggregated with lipid droplets into particles with a rough, jagged morphology due to the incorporation of platelets several hundred nanometres in width into hybrid particles of 2–5 µm in size (shown previously) . Comparatively, SLH particles are comprised of smooth, mostly spherical morphologies due to the small primary particle size of the porous silica nanoparticles …”

“…Since the fabrication technique used to develop SLH particles is simple and versatile, it is possible to develop alternate nanostructured hybrid materials with varying bioactivities toward digestive enzymes . That is, the ability to form particle‐lipid conjugates with comparable three‐dimensional structures is initially controlled by the ability of the specified particles to form Pickering emulsions with lipid‐in‐water droplets .…”

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

“…In addition, there are cases in which interactions between drugs and excipients have unwelcome effects, and the excipients themselves can affect physiological conditions, hence, modulating the fate of the drug in vivo [129]. There was a report about specific interactions between solidification excipient and lipid molecules in both SEDDS formulation and in vivo [30,130,131]. Similar to that, the interactions between a PI and a drug or lipid could influence the performance of SEDDS, including dispersion, lipid digestion, and drug supersaturation, dissolution, and absorption in the GIT.…”

Preparation and Characterization of Paclitaxel/Chitosan Nanosuspensions for Drug Delivery System and Cytotoxicity Evaluation In Vitro

“…Numerous novel chemical compounds discovered in pharmaceutical programs are poorly soluble in water [1][2][3]. In order to obtain appropriate dissolution rates, a decrease in particle size and increase in surface area are usually implemented in various drug delivery systems [4,5]. The use of nanotechnology to achieve a stable nano-sized drug has become a novel strategy and attracted significant attention in recent years [6][7][8].…”

“…With decrease of size and just evenly dispersion in digestion medium (water as model system) the area of contact will be enhanced, favoring saturation solubility and absorption into the target organ consequently [15,17]. On the other hand such a manipulation allows a continuous trend of release, accelerates the effect and corresponding responses, elevates the level of bioavailability and decreases the possible side effects [18,19]. These advantages facilitate the commercial and clinical application of NSn drugs.…”