Nanotechnology Applications for Natural Products Delivery

Part of the Sustainable Agriculture Reviews book series (SARV, volume 44)


Natural products are fascinating molecules in drug discovery for their exciting structure variability and for their interaction with various biological targets, which represent the best approach to develop successful medications for many diseases. The scarce water solubility, low lipophilicity and inappropriate molecular size of many natural compounds, which undergo structural instability in biological milieu, rapid clearance and high metabolic rate, have severely limited their use in clinic. Nanomedicine represents an excellent tool to increase bioavailability and activities of natural products. Generally, nanosized delivery systems provide large surface area increasing dissolution properties and can overcome anatomic barriers. In addition, passive and active targeting can optimize the performance of the nanocarriers. Passive targeting takes advantage of the unique pathophysiological characteristics of inflamed and tumor vessels, enabling nanodrugs to accumulate in the tissues. The effect is called enhanced permeation and retention, generally obtained by the decoration with polyethylene glycol the vector surface. An intriguing strategy is to decorate the nanocarriers with special ligands in order to recognize and bind to target cells through ligand–receptor interactions. Although the active targeting strategy looks intriguing, nanodrugs currently approved for clinical use are relatively simple and generally lack active targeting or triggered drug release components.

In this review different nanocarriers made of polymers or lipid constituents mainly based on artemisinin, curcumin, andrographolide, resveratrol, honokiol, salvianolic acid B, green tea catechins, silymarin and other extracts are reported. Each nanosystem has its own advantages, disadvantages, and characteristics. Polymeric nanoparticles are solid in nature and include nanosphere and nanocapsule. They are ideal candidates to enhance the bioavailability of the natural products after various routes of administration, principally oral and parenteral, but also nasal and intra-ocular, as well as to cross physiological barriers including blood brain barrier. Polymeric micelles have high safety, worthy stability and low cost. Polymeric micelles are very stable in physiological media with a consequent controlled drug release of drugs, while the hydrophilic shell protects the encapsulated drug from the external medium and prevents the interaction with plasma components, resulting in in vivo long circulating properties. Dendrimers are characterized by low polydispersity, good biocompatibility, able to cross cell barriers via both paracellular and transcellular pathways, very versatile able to carry both lipophilic and hydrophilic drugs. Lipid nanocarriers include vesicles, nanocochleates, micelles, solid lipid nanoparticles and nanostructured lipid particles, emulsions with nano scale, including nanoemulsions and microemulsions. Vesicles include liposomes and niosomes are the first nano drug delivery systems that have been successfully translated into real-time clinical applications. They are extremely versatile in terms of route of administration and characteristics of the loaded drug. Due to their similarity to biological membranes provides unique opportunities to deliver drug molecules into cells or subcellular compartments. Liposomes can be converted to nanocochleates, which are unique nanovectors, after treatment with divalent ions, which are very useful for both oral and parenteral administration. Solid lipid nanoparticles and nanostructured lipid particles are easy to scale-up, low cost of production, relative nontoxic nature, biodegradable composition, and stability against aggregation or coalescence. Mostly lipid drugs can be loaded in these nanoparticles to avoid extrusion. Nanoemulsions and microemulsions are the most interesting nanostructures to essentially increase drug loading and enhance bioavailability. They both give reproducible plasma drug profile and can also be used for sustained and targeted drug delivery.


Nanosized delivery systems Natural products Polymeric and lipid nanosystems Bioavailability Efficacy 



The authors acknowledge the funding received from the Department of Chemistry.


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© The Editor(s) (if applicable) and The Author(s), under exclusive license to Springer Nature Switzerland AG 2020

Authors and Affiliations

  1. 1.Department of Chemistry “Ugo Schiff”FlorenceItaly

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