Advances in Nanotechnology for Enhancing the Solubility and Bioavailability of Poorly Soluble Drugs

Figures & data

Figure 1 Biopharmaceutics Classification System (BCS) and Feasible Formulation Choices Based on BCS.

Figure 2 The Basic Principles of Nanodrug Delivery Systems. (A) Working Principles of Nanodrug Delivery Systems. (B) Two structures of liposomes:SLN and NLC. (C) The absorption process of nanodrug delivery systems using SLN as carriers to encapsulate TKIs in the gastrointestinal tract. (D) The advantages of NLC as a carrier for Northaritin. (E) Polymer micelles and vesicles. (F) FA-PGA-PTX micelles can selectively enter FR positive cancer cells through receptor mediated endocytosis. (G) Structural basis of hydrophobic and hydrophilic drugs encapsulated in polymer vesicles. (H) Multiphase nanoemulsion. (I) Enhanced permeability and retention effect. (J) Degradation of nano hydrogel under photochemical conditions. (K) Working Principle of Inorganic Nanocarriers. (L) The Structure and Advantages of Dendritic Polymers.

Figure 3 Mechanism of improving the solubility of insoluble drugs through nano drug delivery systems. (A) Transnasal administration using liposome nanodelivery system. (B) The mechanism of receptor mediated transport and adsorption mediated transport breaking through the blood-brain barrier. (C) Surface modification technology to improve drug targeting. (D) Direct and indirect modification methods. (E) Transferrin and Tamoxifen Modified Polymer Dendritic Polymer PAMAM for the Treatment of Brain Glioma. (F) Carrier mediated technology.

Figure 4 Mechanism of Enhanced Cellular Uptake by Nanomedicine Drug Carriers.

Figure 5 pH-Responsive Mechanism.

Figure 6 Altering Lipid Surface Charge in Nano Drug Delivery Systems.

Figure 7 Mechanism of Phagocytosis Avoidance by PEG-Modified Lipid Molecules.

Figure 8 Physiological Barriers During Drug Delivery to the Target.

Figure 9 Basic Mechanisms of Nanocarrier Action.

Figure 10 Types and Mechanisms of Specific Barriers.

Figure 11 Multifunctional Nanoparticles for Drug Delivery.

Table 1 Key Differences Between Emulsion and Nanoemulsion

Sr.No.	Emulsion	Nanoemulsion
1	Kinetically less stable	Kinetically more stable
2	Appearance-cloudy/opaque	Appearance-clear
3	Particle size varies from 1–1000μm	Particle size varies from 1–100nm
4	Anisotropic in nature	Isotropic in nature
5	Higher surfactant concentration(20–25%)	Lower surfactant concentration(5–10%)
6	Wet gum method and dry gum method are generally used for preparation	High energy emulsification and low energy Emulsification method are used
7	Creaming, Phase inversion, and sedimentation, etc., stability problems may occur.	These types of problems not occur.

Table 2 Selected Exemplary Cases in This Field

Categories	Year of Approval	Pharmaceutical Formulations	Companies	Clinical Applications
Liposomal Nanoparticles	2015	Irinotecan	Merrimack Pharmaceuticals (Cambridge, UK)	Metastatic pancreatic cancer
	2021	Recombinant CSP	ClaxoSmithKline (Middlesex, UK)	Malaria
	2021	BNT162b2	Pfizer (NewYork, NY, USA) and BioNTech (Mainz, Germany)	COVID-19
Polymeric Nanoparticles	2012	Docetaxel	Samyang Pharmaceuticals (Seoul Republic of Korea)	MBC, NSCLC, and ovarian cancer
	2015	PTX	Oasmia Pharmaceuticals (Uppsala, Sweden)	Ovarian cancer
Drug Nanocrystals	2018	Aripiprazole lauroxil	AlkermesInc (Waltham, MA, USA)	Schizophrenia
	2021	Cabotegravir	ViiyHealthcareCo. (Brentford, London, UK)	HIV-1 infection
Other Nanomedicines	2010	Ironmolecule with unbranched carbohydrateinon particles	Pharmacosmos (Rorvangsvei, Holbaek, Denmark)	Iron deficiency anemia
	2013	Polynucleariron (III) oxyhydroxide iron particles	ForInt. (Waltham, MA.USA)	Iron deficiency anemia
	2015	Recombinant anti-hemophilic factor VIII	Baxalta (Montgomery, Al, USA)	Hemophilia A

Abbreviations: FDA, Food and Drug Administration; EMA, European Medicines Agency.