Paeonol-Loaded Ethosomes as Transdermal Delivery Carriers: Design, Preparation and Evaluation

Paeonol exhibits a wide range of pharmacological activities, such as anti-inflammatory, antidiabetic as well as pain-relieving activities. However, its intrinsic properties, such as low water solubility, poor stability and low oral bioavailability, restrict its clinical application. The current study aimed to optimize paeonol-loaded ethosomal formulation and characterize it in terms of encapsulation efficiency (EE), vesicle size (VS), zeta potential (ZP) and polydispersity index (PDI), in addition to differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR) studies. Here, paeonol-loaded ethosomes were prepared by the injection method and optimized by the single-factor test and central composite design-response surface methodology. The optimized paeonol-loaded ethosomes had an EE of 84.33 ± 1.34%, VS of 120.2 ± 1.3 nm, negative charge of −16.8 ± 0.36 mV, and PDI of 0.131 ± 0.006. Ethosomes showed a spherical morphology under the transmission electron microscope (TEM). DSC, XRD and FT-IR results indicated that paeonol was successfully incorporated into the ethosomes. In-vitro transdermal absorption and skin retention of paeonol from paeonol-loaded ethosomes were 138.58 ± 9.60 µg/cm2 and 52.60 ± 7.90 µg/cm2, respectively. With reasonable skin tolerance, ethosomes could be a promising vehicle for transdermal delivery of paeonol.

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The Evaluation of Meloxicam Nanocrystals by Oral Administration with Different Particle Sizes

Molecules ◽

10.3390/molecules27020421 ◽

2022 ◽

Vol 27 (2) ◽

pp. 421

Author(s):

Yao Yu ◽

Yang Tian ◽

Hui Zhang ◽

Qingxian Jia ◽

Xuejun Chen ◽

...

Keyword(s):

Particle Size ◽

Water Solubility ◽

Cell Model ◽

Particle Sizes ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Laser Scattering ◽

Transport Studies ◽

Transmission Electron ◽

Transmission And Absorption

Meloxicam (MLX) is a non-steroidal anti-inflammatory drug used to treat rheumatoid arthritis and osteoarthritis. However, its poor water solubility limits the dissolution process and influences absorption. In order to solve this problem and improve its bioavailability, we prepared it in nanocrystals with three different particle sizes to improve solubility and compare the differences between various particle sizes. The nanocrystal particle sizes were studied through dynamic light scattering (DLS) and laser scattering (LS). Transmission electron microscopy (TEM) was used to characterize the morphology of nanocrystals. The sizes of meloxicam-nanocrystals-A (MLX-NCs-A), meloxicam-nanocrystals-B (MLX-NCs-B), and meloxicam-nanocrystals-C (MLX-NCs-C) were 3.262 ± 0.016 μm, 460.2 ± 9.5 nm, and 204.9 ± 2.8 nm, respectively. Molecular simulation was used to explore the distribution and interaction energy of MLX molecules and stabilizer molecules in water. The results of differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) proved that the crystalline state did not change in the preparation process. Transport studies of the Caco-2 cell model indicated that the cumulative degree of transport would increase as the particle size decreased. Additionally, plasma concentration–time curves showed that the AUC0–∞ of MLX-NCs-C were 3.58- and 2.92-fold greater than those of MLX-NCs-A and MLX-NCs-B, respectively. These results indicate that preparing MLX in nanocrystals can effectively improve the bioavailability, and the particle size of nanocrystals is an important factor in transmission and absorption.

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A Facile Synthesis of Poly(3-octylthiophene)-Titanium Dioxide Nanocomposite Particles in Supercritical CO2

Journal of Nanoscience and Nanotechnology ◽

10.1166/jnn.2008.ic60 ◽

2008 ◽

Vol 8 (9) ◽

pp. 4743-4746 ◽

Cited By ~ 2

Author(s):

Haldorai Yuvaraj ◽

Min Hee Woo ◽

Eun Ju Park ◽

Yeong-Soon Gal ◽

Kwon Taek Lim

Keyword(s):

Titanium Dioxide ◽

Oxidative Polymerization ◽

X Ray Diffraction ◽

Photoluminescence Quenching ◽

Tem Analysis ◽

Ir Studies ◽

Transmission Electron ◽

Ft Ir ◽

Synthesized Materials

Poly(3-octylthiophene) (P3OT)-titanium dioxide (TiO2) nanocomposite powder where TiO2 was embedded with homogeneous dispersion was synthesized by in-situ chemical oxidative polymerization of 3-octylthiophene in the presence of TiO2 nanoparticles in supercritical carbon dioxide (scCO2), using ferric chloride as the oxidant. The synthesized materials could be obtained as dry powder upon venting of CO2 after the polymerization. The composites were subsequently characterized by FT-IR spectroscopy, transmission electron microscopy (TEM), X-ray diffraction studies (XRD), thermogravimetric analysis (TGA) and photoluminescence (PL). The incorporation of TiO2 in the composite was endorsed by FT-IR studies. TGA revealed enhanced thermal stability of P3OT/TiO2 nanocomposite compared to 3-octylthiophene. TEM analysis showed that well dispersed TiO2 nanoparticles in the polymer matrix. Photoluminescence quenching increased with increasing TiO2 concentration in the composite.

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Optical and Structural Properties of PVP/Bi2S3 Nanoparticles by Chemical Method

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.678.248 ◽

2013 ◽

Vol 678 ◽

pp. 248-252

Author(s):

K. Kavi Rasu ◽

Dhandapani Vishnushankar ◽

V. Veeravazhuthi

Keyword(s):

Electron Microscopy ◽

Diffraction Spectrum ◽

X Ray Diffraction ◽

Sem Images ◽

X Ray ◽

Ir Studies ◽

Transmission Electron ◽

Ft Ir ◽

Crystalline Nature ◽

Uv Visible

Bismuth sulfide (Bi2S3) and Polyvinyl pyrrolidone (PVP) encapsulated Bi2S3 Nanoparticles are synthesized from aqueous solutions at room temperature. Synthesized samples are subjected to UV-Visible Spectroscopy, X-Ray Diffraction (XRD), Scanning electron microscopy (SEM), Energy Dispersive Analysis of X-ray (EDAX), Transmission Electron Microscopy (TEM) and FT-IR studies and their results are compared. X-ray diffraction spectrum reveals the crystalline nature of the synthesized samples. Grain size value of PVP/ Bi2S3 nanoparticles show a decrease when compared to Bi2S3 nanoparticles and this ensures the good encapsulant effect of PVP on Bi2S3 nanoparticles. SEM images show that all the particles in the synthesized sample are nearly equal in size. From the TEM image we conclude that the particle size lies between 30nm to 70nm. Finally the samples are subjected to EDAX studies for determining their composition.

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Design and Development of Mupirocin Nanofibers as Medicated Textiles for Treatment of Wound Infection in Secondary Burns

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2021.14.6.4 ◽

2021 ◽

Vol 14 (6) ◽

pp. 5672-5682

Author(s):

Ruchi Tiwari ◽

Akanksha Lahiri ◽

Gaurav Tiwari ◽

Ramachandran Vadivelan

Keyword(s):

High Stability ◽

Solvent Casting ◽

Topical Drug Delivery ◽

Stability Studies ◽

Scanning Calorimetry ◽

Electrospinning Technique ◽

Ir Studies ◽

Permeation Studies ◽

Ft Ir

The present study assessed the topical potential of nanofibers loaded with Mupirocin (MUP) for the treatment of burns. Nanofibers of MUP were composed of Polyvinyl Pyrrolidone (PVP), Gelatin Type-A, and Ethanol using two methods: Solvent casting and Electrospinning. Nanofibers were characterized for Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), Differential scanning calorimetry (DSC), Thermogravimetric analysis (TGA), Drug Content Studies, in-vitro drug permeation, antibacterial and stability studies. The FT-IR studies showed that the Electrospinning technique had a very good mixing of MUP with the polymer. SEM studies showed that the morphology of electrospinning nanofibers had diameters in the range of 70.41 nm- 406.83 nm. The thermal decomposition studies of optimized Nanofiber (E.S.1) were performed by DSC and TGA study and it was found that the formulation had high stability in high-temperature environments. Permeation studies showed that E.S.1 had the highest percentage amount and controlled release of the drug (90 %) up to 8 has compared to other formulations. Nanofibers prepared through the Electrospinning technique showed better antibacterial activity against Staphylococcus aureus as compared to the Solvent casting nanofibers. This research suggested that MUP loaded nanofibers can be potentially used as a topical drug delivery system for the treatment of burns.

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Consequence of ANASTROZOLE on Chemo therapy

Cancer Research and Cellular Therapeutics ◽

10.31579/2640-1053/013 ◽

2017 ◽

Vol 1 (2) ◽

pp. 01-04

Author(s):

Saritha Garrepalli

Keyword(s):

Particle Size ◽

In Vitro Release ◽

Scanning Calorimetry ◽

Ir Studies ◽

Release Studies ◽

Ft Ir ◽

The Mean ◽

Pure Drug ◽

The Stability

Prepared nanoparticles were characterized in terms of particle size, scanning electron microscope (SEM), fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). In-vitro release studies were performed in phosphate buffer saline pH 7.4 at 37˚±0.5˚C for 1month. The mean particle size of obtained nanoparticles was 150-400 nm and was apparently spherical in shape, with smooth surface. DSC is done for the stability test for pure drug and sample. The thermogram of drug has not shifted for in the formulation compare to pure drug thermogram hence, the stability of formulation is not changed. FT-IR studies demonstrated that the drug was not changed in the formulation during the fabrication process.The encapsulation efficiency was about 48%. The Anastrozole-BSA nanoparticles exhibit a most interesting release profile with small initial burst followed by slower and controlled release.

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Two Novel Palbociclib-Resorcinol and Palbociclib-Orcinol Cocrystals with Enhanced Solubility and Dissolution Rate

Pharmaceutics ◽

10.3390/pharmaceutics14010023 ◽

2021 ◽

Vol 14 (1) ◽

pp. 23

Author(s):

Chenxin Duan ◽

Wenwen Liu ◽

Yunwen Tao ◽

Feifei Liang ◽

Yanming Chen ◽

...

Keyword(s):

Water Solubility ◽

Cancer Drug ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Dissolution Rates ◽

Intrinsic Dissolution ◽

X Ray ◽

Enhanced Solubility

Palbociclib (PAL) is an effective anti-breast cancer drug, but its use has been partly restricted due to poor bioavailability (resulting from extremely low water solubility) and serious adverse reactions. In this study, two cocrystals of PAL with resorcinol (RES) or orcinol (ORC) were prepared by evaporation crystallization to enhance their solubility. The cocrystals were characterized by single crystal X-ray diffraction, Hirshfeld surface analysis, powder X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared and scanning electron microscopy. The intrinsic dissolution rates of the PAL cocrystals were determined in three different dissolution media (pH 1.0, pH 4.5 and pH 6.8), and both cocrystals showed improved dissolution rates at pH 1.0 and pH 6.8 in comparison to the parent drug. In addition, the cocrystals increased the solubility of PAL at pH 6.8 by 2–3 times and showed good stabilities in both the accelerated stability testing and stress testing. The PAL-RES cocrystal also exhibited an improved relative bioavailability (1.24 times) than PAL in vivo pharmacokinetics in rats. Moreover, the in vitro cytotoxicity assay of PAL-RES showed an increased IC50 value for normal cells, suggesting a better biosafety profile than PAL. Co-crystallization may represent a promising strategy for improving the physicochemical properties of PAL with better pharmacokinetics.

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In Vitro Antifungal Activity and Mechanism of Ag3PW12O40 Composites against Candida Species

Molecules ◽

10.3390/molecules25246012 ◽

2020 ◽

Vol 25 (24) ◽

pp. 6012

Author(s):

Xinming Zhang ◽

Tianzhan Zhang ◽

Shuanli Guo ◽

Yang Zhang ◽

Rongtian Sheng ◽

...

Keyword(s):

Minimum Inhibitory Concentration ◽

Candida Species ◽

Inhibitory Concentration ◽

Fungal Infections ◽

Positive Control ◽

X Ray Diffraction ◽

Transmission Electron ◽

Microbial Infections ◽

Ft Ir

Fungal infections pose a serious threat to human health. Polyoxometalates (POMs) are metal–oxygen clusters with potential application in the control of microbial infections. Herein, the Ag3PW12O40 composites have been synthesized and verified by Fourier transform infrared (FT-IR) spectrum, transmission electron microscopy (TEM), scanning electron microscope (SEM), elemental analysis, and X-ray diffraction (XRD). The antifungal activities of Ag3PW12O40 were screened in 19 Candida species strains through the determination of minimum inhibitory concentration (MIC) by the microdilution checkerboard technique. The minimum inhibitory concentration (MIC50) values of Ag3PW12O40 are 2~32 μg/mL to the Candida species. The MIC80 value of Ag3PW12O40 to resistant clinical isolates C. albicans HL963 is 8 μg/mL, which is lower than the positive control, fluconazole (FLC). The mechanism against C. albicans HL963 results show that Ag3PW12O40 can decrease the ergosterol content. The expressions of ERG1, ERG7, and ERG11, which impact on the synthesis of ergosterol, are all prominently upregulated by Ag3PW12O40. It indicates that Ag3PW12O40 is a candidate in the development of new antifungal agents.

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A Green Approach for the Synthesis of a Cerium Oxide Nanoparticle: Characterization and Antibacterial Activity

International Journal of Nanoscience ◽

10.1142/s0219581x14500185 ◽

2014 ◽

Vol 13 (03) ◽

pp. 1450018 ◽

Cited By ~ 50

Author(s):

S. K. Kannan ◽

M. Sundrarajan

Keyword(s):

Electron Microscope ◽

Cerium Oxide ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Thermo Gravimetric ◽

X Ray ◽

Green Approach ◽

Transmission Electron ◽

Ft Ir ◽

Oxide Nanoparticle

In this study, the synthesis of a cerium oxide nanoparticle was carried out from Acalypha indica leaf extract. The synthesized nanoparticle was characterized by using X-ray diffraction (XRD), Scanning Electron Microscope (SEM), Energy Dispersive X-ray (EDX) and Transmission Electron Microscope (TEM) for structural confirmation. The studies clearly indicate that the synthesized CeO 2 nanoparticle is a crystalline material with particle size between 25–30 nm. Further analysis was carried out by Fourier Transform infrared spectroscopy (FT-IR), to provide evidence for the presence of Ce - O - Ce asymmetry stretching of the CeO 2 nanoparticle. Thermo Gravimetric and Differential Scanning Calorimetry analyses gave the thermal properties of cerium oxide nanoparticles. Antibacterial studies were conducted using the synthesized CeO 2. This result showed increasing rate of antibacterial behavior with gram positive and gram negative bacteria.

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Study of ZnO-CNT Nanocomposites in High-Pressure Conditions

Materials ◽

10.3390/ma14185330 ◽

2021 ◽

Vol 14 (18) ◽

pp. 5330

Author(s):

Laura-Madalina Cursaru ◽

Sorina Nicoleta Valsan ◽

Maria-Eliza Puscasu ◽

Ioan Albert Tudor ◽

Nicoleta Zarnescu-Ivan ◽

...

Keyword(s):

Electron Microscopy ◽

High Pressure ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

X Ray ◽

Transmission Electron ◽

Specific Morphology ◽

Ft Ir ◽

Nanocomposite Powders

Recently, carbon nanotubes (CNTs) have been used extensively to develop new materials and devices due to their specific morphology and properties. The reinforcement of different metal oxides such as zinc oxide (ZnO) with CNT develops advanced multifunctional materials with improved properties. Our aim is to obtain ZnO-CNT nanocomposites by in situ hydrothermal method in high-pressure conditions. Various compositions were tested. The structure and morphology of ZnO-CNT nanocomposites were analyzed by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry—thermogravimetry (DSC-TG), X-ray diffraction (XRD), scanning electron microscopy (SEM), energy dispersive X-ray spectroscopy (EDX), and transmission electron microscopy (TEM). These analyses showed the formation of complex ZnO-CNT structures. FT-IR spectra suggest possible interactions between CNT and ZnO. DSC-TG analysis also reveals the formation of some physical bonds between ZnO and CNT, through the appearance of endothermic peaks which could be assigned to the decomposition of functional groups of the CNT chain and breaking of the ZnO-CNT bonds. XRD characterization demonstrated the existence of ZnO nanocrystallites with size around 60 nm. The best ZnO:CNT composition was further selected for preliminary investigations of the potential of these nanocomposite powders to be processed as pastes for extrusion-based 3D printing.

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Mechanochemical Synthesis and Physicochemical Characterization of Previously Unreported Praziquantel Solvates with 2-Pyrrolidone and Acetic Acid

Pharmaceutics ◽

10.3390/pharmaceutics13101606 ◽

2021 ◽

Vol 13 (10) ◽

pp. 1606

Author(s):

Debora Zanolla ◽

Lara Gigli ◽

Dritan Hasa ◽

Michele R. Chierotti ◽

Mihails Arhangelskis ◽

...

Keyword(s):

Acetic Acid ◽

Water Solubility ◽

Physicochemical Characterization ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Pxrd Pattern ◽

Intrinsic Dissolution ◽

Ft Ir ◽

Biopharmaceutical Properties

Two new solvates of the widely used anthelminthic Praziquantel (PZQ) were obtained through mechanochemical screening with different liquid additives. Specifically, 2-pyrrolidone and acetic acid gave solvates with 1:1 stoichiometry (PZQ-AA and PZQ-2P, respectively). A wide-ranging characterization of the new solid forms was carried out by means of powder X-ray diffraction, differential scanning calorimetry, FT-IR, solid-state NMR and biopharmaceutical analyses (solubility and intrinsic dissolution studies). Besides, the crystal structures of the two new solvates were solved from their Synchrotron-PXRD pattern: the solvates are isostructural, with equivalent triclinic packing. In both structures acetic acid and 2-pyrrolidone showed a strong interaction with the PZQ molecule via hydrogen bond. Even though previous studies have shown that PZQ is conformationally flexible, the same syn conformation as the PZQ Form A of the C=O groups of the piperazinone-cyclohexylcarbonyl segment is involved in these two new solid forms. In terms of biopharmaceutical properties, PZQ-AA and PZQ-2P exhibited water solubility and intrinsic dissolution rate much greater than those of anhydrous Form A.

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