http://if-pan.krakow.pl/pjp/pdf/2012/5_1020.pdf

Nanoparticles as drug delivery systems

Nanoparticle-liver interactions: Cellular uptake and hepatobiliary elimination

Gelatin-based nanoparticles as drug and gene delivery systems: reviewing three decades of research.

Polymeric nanoparticles: Promising platform for drug delivery.

In the last decades, the discovery of metabolites from marine resources showing biological activity has increased significantly. Among marine resources, seaweed is a valuable source of structurally diverse bioactive compounds. The cell walls of marine algae are rich in sulfated polysaccharides, including carrageenan in red algae, ulvan in green algae and fucoidan in brown algae. Sulfated polysaccharides have been increasingly studied over the years in the pharmaceutical field, given their potential usefulness in applications such as the design of drug delivery systems. The purpose of this review is to discuss potential applications of these polymers in drug delivery systems, with a focus on carrageenan, ulvan and fucoidan. General information regarding structure, extraction process and physicochemical properties is presented, along with a brief reference to reported biological activities. For each material, specific applications under the scope of drug delivery are described, addressing in privileged manner particulate carriers, as well as hydrogels and beads. A final section approaches the application of sulfated polysaccharides in targeted drug delivery, focusing with particular interest the capacity for macrophage targeting.

https://www.mdpi.com/1660-3397/14/3/42/pdf

Sulfated Seaweed Polysaccharides as Multifunctional Materials in Drug Delivery Applications.

Gelatin nanocarriers as potential vectors for effective management of tuberculosis

The objective of the present study was to evaluate the prospective of engineered nanoparticles for selective delivery of an antituberculosis drug, rifabutin, to alveolar tissues. Drug-loaded solid lipid nanoparticles (SLNs) were synthesized and efficiently mannosylated. The formation of uncoated and coated SLNs was characterized by FTIR spectroscopy and SEM studies. A variety of physicochemical parameters such as drug loading, particle size, polydispersity index, zeta potential, and in vitro drug release were determined. The toxicity and targeting potential of the prepared formulation were assessed with alveolar macrophage uptake, hematological studies, and in vivo studies of uncoated and coated SLNs. Ex vivo cellular uptake studies of SLNs formulations in alveolar macrophages depicted almost six times enhanced uptake due to mannose coating. The hematological studies proved mannose-conjugated system to be less immunogenic and suitable for sustained delivery as evaluated against uncoated formulation. Further, the serum level and organ distribution studies demonstrated efficiency of the system for prolonged circulation and spatial delivery of rifabutin to alveolar tissues. Finally, it was concluded that mannose-conjugated SLNs can be exploited for effective and targeted delivery of rifabutin compared to its uncoated formulation and ultimately increasing the therapeutic margin of safety while reducing the side effects.

Mannosylated nanoparticulate carriers of rifabutin for alveolar targeting

The mannosylated gelatin nanoparticles (Mn-GNPs) were prepared for the selective delivery of an antitubercular drug, isoniazid (INH), to the alveolar macrophages. The gelatin nanoparticles (GNPs) were prepared by using a two-step desolvation method and efficiently conjugated with mannose. Various parameters such as particle size, polydispersity index, zeta potential, % entrapment efficiency, in vitro drug release, macrophage uptake, in vivo biodistribution, antitubercular activity and hepatotoxicity of plain and Mn-GNPs were determined. The size of nanoparticles (both plain and Mn-GNPs) was found to be in range of 260–380 nm, and maximum drug payload was found to be 40–55%. Average particle size of Mn-GNPs was more, whereas drug entrapment was lesser compared to plain GNPs. The organ distribution studies demonstrated the efficiency of Mn-GNPs for spatial delivery of INH to alveolar tissues. Intravenous administration of INH loaded Mn-GNPs (I-Mn-GNPs) resulted in significant reduction in bacterial counts i...

Mannosylated gelatin nanoparticles bearing isoniazid for effective management of tuberculosis.

The attempts to oral delivery of lipids can be challenging. Self-emulsifying drug delivery system (SEDDS) plays a vital role to tackle this problem. SEDDS is composed of an oil phase, surfactants, co-surfactants, emulsifying agents, and co-solvents. SEDDS can be categorized into self-nano-emulsifying agents (SNEDDS) and self-micro-emulsifying agents (SMEDDS). The characterization of SEDDS includes size, zeta potential analysis, and surface morphology via electron microscopy and phase separation methods. SEDDS can be well characterized through different techniques for size and morphology. Supersaturation is the phenomenon applied in case of SEDDS, in which polymers and copolymers are used for SEDDS preparation. A supersaturated SEDDS formulation kinetically and thermodynamically inhibits the precipitation of drug molecules by retarding nucleation and crystal growth in the aqueous medium. Self-emulsification approach has been successful in the delivery of anti-cancer agents, anti-viral drugs, anti-bacterial, immunosuppressant, and natural products such as antioxidants as well as alkaloids. At present, more than four SEDDS drug products are available in the market. SEDDS have tremendous capabilities which are yet to be explored which would be beneficial in oral lipid delivery.

Self-Emulsifying Oral Lipid Drug Delivery Systems: Advances and Challenges.

Blood Brain Barrier (BBB) represents a major hurdle for the delivery of bioactives in the brain. It serves as a major constraint for the entry of hydrophilic drugs and the efflux pumps present on its surface restrain the intracellular accumulation of pharmacological moieties in the brain. Nanoparticles (NPs) in this regard can serve as a potential module for ferrying large doses of drugs across the BBB. These can be coated at surfaces or fabricated with a targeting moiety, so as to gain access in the brain thus, minimizing the toxicity of therapy. Therefore, the NPs can serve as an exclusive dais for spatial and temporal distribution of pharmacological agents across the brain, escalating the probability of disease free survival. The current review explores the various possible mechanisms so that the NPs can gain access in the brain viz a viz adsorption, receptor mediated endocytosis, transcytosis, inhibiting p-glycoprotein efflux pump, membrane permeabilization effect and disrupting the BBB. The article also accounts the prospects of NPs to enhance the transport of therapeutic agents across the brain, providing refined drug delivery.

Gaurav K. Saraogi

Papers

Gelatin nanocarriers as potential vectors for effective management of tuberculosis

Mannosylated nanoparticulate carriers of rifabutin for alveolar targeting

Mannosylated gelatin nanoparticles bearing isoniazid for effective management of tuberculosis.

Self-Emulsifying Oral Lipid Drug Delivery Systems: Advances and Challenges.

Nanoparticles as novel carrier for brain delivery: a review.