Nanocrystals Technology for Transdermal Delivery of Water-Insoluble Drugs

Liu, Yangyang; Zhao, Juan; Wang, Lulu; Yan, Beibei; Gu, Yu; Chang, Ping; Wang, Yancai

doi:10.2174/1567201815666180518124345

Cited by 20 publications

(12 citation statements)

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“…In this regard, nanocrystal technology has been introduced as a noteworthy route for transdermal delivery of the water‐insoluble drugs. Due to the low bioavailability of rutin, this method could be beneficial for its transdermal delivery (Liu et al, 2018).…”

Section: Therapeutic Benefits Of Rutin and Its Nanoformulationsmentioning

confidence: 99%

Therapeutic benefits of rutin and its nanoformulations

Negahdari

Bohlouli

Sharifi

et al. 2020

Phytotherapy Research

152

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Background Rutin as a natural flavonoid compound has revealed an extensive range of therapeutic potentials. Purpose The current paper is focused on the numerous studies on rutin nanoformulations regarding its broad spectrum of therapeutic potentials. Study and methods A review was conducted in electronic databases (PubMed) to identify relevant published literature in English. No restrictions on publication date were imposed. Results The literature search provided 7,078 results for rutin. Among them, 25 papers were related to the potential biological activities of rutin nanoformulations. Polymeric nanoparticles were the most studied nanoformulations for rutin (14 titles) and lipid nanoparticles (5 titles) were in second place. The reviewed literature showed that rutin has been used as an antimicrobial, antifungal, and anti‐allergic agent. Improving the bioavailability of rutin using novel drug‐delivery methods will help the investigators to use its useful effects in the treatment of various chronic human diseases. Conclusion It can be concluded that the preparation of rutin nanomaterials for the various therapeutic objects confirmed the enhanced aqueous solubility as well as enhanced efficacy compared to conventional delivery of rutin. However, more investigations should be conducted to confirm the improved bioavailability of the rutin nanoformulations.

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Section: Therapeutic Benefits Of Rutin and Its Nanoformulationsmentioning

confidence: 99%

Therapeutic benefits of rutin and its nanoformulations

Negahdari

Bohlouli

Sharifi

et al. 2020

Phytotherapy Research

152

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“…Table 3. pKa values of GA, binary solid dispersion (BSD), meglumine ternary solid dispersion (MG-TSD), and L-arginine ternary solid dispersion (LA-TSD) obtained from Equation (1). SEM was used to observe the changes in the surface morphology of the materials.…”

Section: Dissociation Constant (Pka)mentioning

confidence: 99%

“…At present, most widely used drugs, natural products, and drug candidates are insoluble in water, and increasing the solubility of poorly soluble drugs is an important problem for many drug molecules [1][2][3]. Several strategies have been studied to overcome this problem, such as salt formation [4][5][6], nanoparticles [7][8][9][10], inclusion complexes [11], liposomes [12,13], and amorphous solid dispersions [14][15][16][17].…”

Section: Introductionmentioning

confidence: 99%

Mechanism and Improved Dissolution of Glycyrrhetinic Acid Solid Dispersion by Alkalizers

et al. 2020

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The purpose of this study was to increase the dissolution of glycyrrhetinic acid (GA) by preparing ternary solid dispersion (TSD) systems containing alkalizers, and to explore the modulating mechanism of alkalizers in solid dispersion systems. GA TSDs were prepared by hot melt extrusion (HME) with Kollidon® VA64 as the carrier and L-arginine/meglumine as the alkalizers. The in vitro release of the TSD was investigated with a dissolution test, and the dissociation constant (pKa) was used to describe the ionization degree of the drug in different pH buffers. Scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Fourier Transform Infrared Spectroscopy (FTIR), Raman spectra, X-ray photoelectron spectroscopy (XPS), and a molecular model were used for solid-state characterizations and to study the dissolution mechanism of the TSDs. It was evident that the dissolution of GA significantly increased as a result of the TSD compared to the pure drug and binary solid dispersion. SEM, DSC, and XPRD data showed that GA transformed into an amorphous form in TSD. As illustrated by FTIR, Raman, XPS, and molecular docking, high binding energy ion-pair complexes formed between GA and the alkalizers during the process of HME. These can destroy the H-bond between GA molecules. Further, intermolecular H-bonds formed between the alkalizers and Kollidon® VA64, which can increase the wettability of the drug. Our results will significantly improve the solubility and dissolution of GA. In addition, the lower pKa value of TSD indicates that higher ionization is beneficial to the dissolution of the drug. This study should facilitate further developments of TSDs containing alkalizers to improve the dissolution of weakly acidic drugs and gain a richer understanding of the mechanism of dissolution.

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“…As an effective method of drug delivery, the microparticle drug delivery system has been widely concerned. [12][13][14][15] Nano-carriers have many advantages when carrying drugs, such as higher biocompatibility and lower biotoxicity, controlled drug release, protection of drugs from the external environment, and promotion of oral absorption. [16][17][18][19][20] Moreover, the surface of nano-carriers can also be modified with polymers to achieve targeted drug delivery, reduced drug dose, improved physicochemical properties of drugs, and enhanced the therapeutic effect.…”

Section: Introductionmentioning

confidence: 99%

Mechanism of Enhanced Oral Absorption of a Nano-Drug Delivery System Loaded with Trimethyl Chitosan Derivatives

Zhao¹,

Lin²,

Fang³

et al. 2022

IJN

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Introduction In the previous study, nanoparticles coated with trimethyl chitosan (TMC) derivatives (PPTT-NPs) could promote the oral bioavailability of panax notoginseng saponins (PNS). Herein, we chose PPTT-NPs as a model drug to study the property and mechanism of intestinal absorption in vitro and in vivo. Methods The stability of PPTT-NPs was evaluated using simulated gastric fluid and simulated intestinal fluid. The uptake and transport of PPTT-NPs were investigated in Caco-2 and Caco-2&HT29 co-culture cells. The biosafety, intestinal permeability, adhesion, and absorption mechanism of PPTT-NPs were investigated using SD rats in vivo. The live imaging and biodistribution of PPTT-NPs were observed by IVIS. Furthermore, the effects on CYP3A4 of PPTT-NPs were investigated using testosterone as the probe substrate. Results The results of the stability assay showed that PPTT-NPs had a strong tolerance to the pH and digestive enzymes in the gastrointestinal environment. In vitro cell experiments showed that the uptake of drugs exhibited a time-dependent. When the ratio of TMC-VB 12 and TMC-Cys was 1:3, the uptake capacity of PPTT-NPs was the highest. PPTT-NPs could enhance the paracellular transport of drugs by reversibly opening a tight junction. Animal experiments demonstrated that PPTT-NPs have good biological safety. PPTT-NPs had good adhesion and permeability to small intestinal mucosa. Meanwhile, PPTT-NPs needed energy and various protein to participate in the uptake of drugs. The live imaging of NPs illustrated that PPTT-NPs could prolong the residence time in the intestine. Moreover, TMC-VB 12 and TMC-Cys could reduce the metabolism of drugs by inhibiting CYP3A4 to a certain extent. Conclusion The results show that TMC-VB 12 and TMC-Cys are effective in the transport of PPTT-NPs. PPTT-NPs can increase the intestinal adhesion of drugs and exert high permeation by intestinal enterocytes which demonstrate significant and efficient potential for oral delivery of the BCS III drugs.

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Nanocrystals Technology for Transdermal Delivery of Water-Insoluble Drugs

Cited by 20 publications

References 0 publications

Therapeutic benefits of rutin and its nanoformulations

Therapeutic benefits of rutin and its nanoformulations

Mechanism and Improved Dissolution of Glycyrrhetinic Acid Solid Dispersion by Alkalizers

Mechanism of Enhanced Oral Absorption of a Nano-Drug Delivery System Loaded with Trimethyl Chitosan Derivatives

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