Resveratrol Encapsulation and Release from Pristine and Functionalized Mesoporous Silica Carriers

Resveratrol, a naturally occurring polyphenol, has attracted significant attention due to its antioxidant, cardioprotective and anticancer potential. However, its low aqueous solubility limits resveratrol bioavailability and use. In this work, different mesoporous silica matrices were used to encapsulate the polyphenol and to increase its dissolution rate. Pristine MCM-41, MCM-48, SBA-15, SBA-16, FDU-12 and MCF silica were obtained. The influence of SBA-15 functionalized with aminopropyl, isocyanate, phenyl, mercaptopropyl, and propionic acid moieties on resveratrol loading and release profiles was also assessed. The cytotoxic effects were evaluated for mesoporous carriers and resveratrol-loaded samples against human lung cancer (A549), breast cancer (MDA-MB-231) and human skin fibroblast (HSF) cell lines. The effect on apoptosis and cell cycle were assayed for selected resveratrol-loaded carriers. The polyphenol molecules are encapsulated only inside the mesopores, mostly in amorphous state. All materials containing either pristine or functionalized silica carriers increased polyphenol dissolution rate. The influence of the physico-chemical properties of the mesoporous carriers and resveratrol–loaded supports on the kinetic parameters was identified. Resv@SBA-15-SH and Resv@SBA-15-NCO samples exhibited the highest anticancer effect against A549 cells (IC50 values were 26.06 and 36.5 µg/mL, respectively) and against MDA-MB-231 (IC50 values were 35.56 and 19.30 µg/mL, respectively), which highlights their potential use against cancer.

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Effect of an Albumin-Coated Mesoporous Silicon Nanoparticle Platform for Paclitaxel Delivery in Human Lung Cancer Cell Line A549

Journal of Nanomaterials ◽

10.1155/2016/4086456 ◽

2016 ◽

Vol 2016 ◽

pp. 1-9 ◽

Cited By ~ 1

Author(s):

Yu Gao ◽

Xiaofang Che ◽

Chunlei Zheng ◽

Kezuo Hou ◽

Xiujuan Qu ◽

...

Keyword(s):

Lung Cancer ◽

Dissolution Rate ◽

Laser Scanning ◽

Silicon Nanoparticles ◽

A549 Cells ◽

Amorphous State ◽

Lung Cancer Cell Line ◽

Human Lung Cancer ◽

Absorption Mechanism ◽

Mesoporous Silicon

Albumin-coated paclitaxel-mesoporous silicon nanoparticles (APMSN) were prepared to improve the anticancer effect in lung cancer by means of regulating the dissolution rate of paclitaxel (PTX). PTX was absorbed into the mesoporous structure of mesoporous silicon nanoparticles (MSN), which was defined as PMSN. PTX was proved to exist in an amorphous state in PMSN, which increased the dissolution rate of PTX. Albumin was coated on the surface of MSN to form AMSN; AMSN and PTX were mixed to form APMSN in order to achieve sustained release of PTX. Then, it was found that APMSN had more significant antiproliferate effects and induced more apoptotic proportion in comparison with PTX in A549 cells. Furthermore, the absorption mechanism of APMSN into A549 cells was investigated. Transmission electron microscopy (TEM) and laser scanning confocal microscopy (LSCM) showed that APMSN could cross the cell membrane and was taken into the cytoplasm quickly. Taken together, our results demonstrate that AMSN carriers have potential as nanodrug delivery systems in the treatment of lung cancer.

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Amine-Functionalized Mesoporous Silica Nanoparticles: A New Nanoantibiotic for Bone Infection Treatment

Biomedical glasses ◽

10.1515/bglass-2017-0011 ◽

2017 ◽

Vol 3 (1) ◽

Cited By ~ 1

Author(s):

Daniel Pedraza ◽

Jaime Díez ◽

Isabel Izquierdo-Barba ◽

Montserrat Colilla ◽

María Vallet-Regí

Keyword(s):

Mesoporous Silica ◽

Silica Nanoparticles ◽

Mesoporous Silica Nanoparticles ◽

Chemical Properties ◽

Bone Infection ◽

Bacterial Biofilm ◽

Functionalized Mesoporous Silica ◽

Transmission Electron ◽

Infection Treatment ◽

Physical And Chemical

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Solubility, Permeability, and Dissolution Rate of Naftidrofuryl Oxalate Based on BCS Criteria

Pharmaceutics ◽

10.3390/pharmaceutics12121238 ◽

2020 ◽

Vol 12 (12) ◽

pp. 1238

Author(s):

Marta Kus-Slowinska ◽

Monika Wrzaskowska ◽

Izabela Ibragimow ◽

Piotr Igor Czaklosz ◽

Anna Olejnik ◽

...

Keyword(s):

Dissolution Rate ◽

Chemical Properties ◽

Aqueous Solubility ◽

Immediate Release ◽

Drug Substances ◽

High Dissolution Rate ◽

Cerebral Diseases ◽

Preliminary Classification

The Biopharmaceutics Classification System (BCS) was conceived to classify drug substances by their in vitro aqueous solubility and permeability properties. The essential activity of naftidrofuryl oxalate (NF) has been described as the inhibition of the serotonin receptors (5-HT2), resulting in vasodilation and decreasing blood pressure. Since the early 1980s, NF has been used to treat several venous and cerebral diseases. There is no data available on the BCS classification of NF. However, based on its physical-chemical properties, NF might be considered to belong to the 1st or the 3rd BCS class. The present study aimed to provide data concerning the solubility and permeability of NF through Caco-2 monolayers and propose its preliminary classification into BCS. We showed that NF is a highly soluble and permeable drug substance; thus, it might be suggested to belong to BCS class I. Additionally, a high dissolution rate of the encapsulated NF based on Praxilene® 100 mg formulation was revealed. Hence, it might be considered as an immediate-release (IR).

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Enhancing the aqueous solubility and dissolution of olanzapine using freeze-drying

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502011000400011 ◽

2011 ◽

Vol 47 (4) ◽

pp. 743-749 ◽

Cited By ~ 7

Author(s):

Mudit Dixit ◽

Ashwini Gopalkrishna Kini ◽

Parthasarthi Keshavarao Kulkarni

Keyword(s):

Dissolution Rate ◽

Freeze Drying ◽

Physical Stability ◽

Amorphous State ◽

Aqueous Solubility ◽

Water Soluble ◽

Freeze Dried ◽

Poorly Water Soluble ◽

Pure Drug ◽

Stability Results

The aim of the present study was to develop an olanzapine freeze-dried tablet (FDT). The solubility and dissolution rate of poorly water-soluble olanzapine was improved by preparing a freeze-dried tablet of olanzapine using the freeze-drying technique . The FDT was prepared by dispersing the drug in an aqueous solution of highly water-soluble carrier materials consisting of gelatin, glycine, and sorbitol. The mixture was poured in to the pockets of blister packs and then was subjected to freezing and lyophilisation. The FDT was characterised by DSC, XRD and SEM and was evaluated for saturation solubility and dissolution. The samples were stored in a stability chamber to investigate their physical stability. Results obtained by DSC and X-ray were analysed and showed the crystalline state of olanzapine in FDT transformation to the amorphous state during the formation of FDT. Scanning electron microscope (SEM) results suggest reduction in olanzapine particle size. The solubility of olanzapine from the FDT was observed to be nearly four and a half times greater than the pure drug. Results obtained from dissolution studies showed that olanzapine FDT significantly improved the dissolution rate of the drug compared with the physical mixture (PM) and the pure drug. More than 90% of olanzapine in FDT dissolved within 5 minutes, compared to only 19.78% of olanzapine pure drug dissolved over the course of 60 minutes. In a stability test, the release profile of the FDT was unchanged, as compared to the freshly prepared FDT after 90 days of storing.

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Biodegradable Alginate-Chitosan Hollow Nanospheres for Codelivery of Doxorubicin and Paclitaxel for the Effect of Human Lung Cancer A549 Cells

BioMed Research International ◽

10.1155/2018/4607945 ◽

2018 ◽

Vol 2018 ◽

pp. 1-11 ◽

Cited By ~ 12

Author(s):

Liu Tao ◽

Jie Jiang ◽

Yu Gao ◽

Chao Wu ◽

Ying Liu

Keyword(s):

Lung Cancer ◽

Human Lung ◽

Hollow Structure ◽

A549 Cells ◽

Amorphous State ◽

Cell Uptake ◽

Human Lung Cancer ◽

Scanning Calorimetry ◽

Adsorption Method ◽

Multiple Drugs

A biodegradable alginate coated chitosan hollow nanosphere (ACHN) was prepared by a hard template method and used for codelivery of doxorubicin (DOX) and paclitaxel (PTX) to investigate the effect on human lung cancer A549 cells. PTX was loaded into the nanometer hollow structure of ACHN through adsorption method. DOX was coated on surface of ACHN through electrostatic interaction. Drug release studies exhibited a sustained-release effect. According to X-ray diffraction patterns (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR) analysis, DOX structure in the loading samples (DOX-PTX-ACHN) was of amorphous state while PTX was microcrystalline. Cytotoxicity experiments showed ACHN was nontoxic as carrier material and the combination of DOX and PTX in DOX-PTX-ACHN exhibited a good inhibiting effect on cell proliferation. Cell uptake experiments demonstrated that DOX-PTX-ACHN accumulated in the cytoplasm. Degradation experiments illustrated that ACHN was a biodegradable material. In summary, these results clearly indicate that ACHN can be utilized as a potential biomaterial to transport multiple drugs to be used in combination therapy.

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Identifying a Membrane-Type 2 Matrix Metalloproteinase-Targeting Peptide for Human Lung Cancer Detection and Targeting Chemotherapy with Functionalized Mesoporous Silica

ACS Applied Bio Materials ◽

10.1021/acsabm.8b00633 ◽

2018 ◽

Vol 2 (1) ◽

pp. 397-405 ◽

Cited By ~ 1

Author(s):

Li Ren ◽

Zheng Ma ◽

Qinglan Li ◽

Weidong Zhao ◽

Ye Wang ◽

...

Keyword(s):

Lung Cancer ◽

Mesoporous Silica ◽

Cancer Detection ◽

Human Lung ◽

Human Lung Cancer ◽

Functionalized Mesoporous Silica ◽

Targeting Peptide ◽

Membrane Type ◽

Lung Cancer Detection

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Amine-Functionalized Mesoporous Silica Nanoparticles: A New Nanoantibiotic for Bone Infection Treatment

Biomedical glasses ◽

10.1515/bglass-2018-0001 ◽

2018 ◽

Vol 4 (1) ◽

pp. 1-12 ◽

Cited By ~ 17

Author(s):

Daniel Pedraza ◽

Jaime Díez ◽

Isabel-Izquierdo-Barba ◽

Montserrat Colilla ◽

María Vallet-Regí

Keyword(s):

Mesoporous Silica ◽

Silica Nanoparticles ◽

Mesoporous Silica Nanoparticles ◽

Chemical Properties ◽

Bone Infection ◽

Bacterial Biofilm ◽

Functionalized Mesoporous Silica ◽

Infection Treatment ◽

Antimicrobial Effectiveness

Abstract This manuscript reports an effective new alternative for the management of bone infection by the development of an antibiotic nanocarrier able to penetrate bacterial biofilm, thus enhancing antimicrobial effectiveness. This nanosystem, also denoted as “nanoantibiotic”, consists in mesoporous silica nanoparticles (MSNs) loaded with an antimicrobial agent (levofloxacin, LEVO) and externally functionalized with N-(2-aminoethyl)-3- aminopropyltrimethoxysilane (DAMO) as targeting agent. This amine functionalization provides MSNs of positive charges, which improves the affinity towards the negatively charged bacteria wall and biofilm. Physical and chemical properties of the nanoantibiotic were studied using different characterization techniques, including Xray diffraction (XRD), transmission electron microscopy (TEM), N2 adsorption porosimetry, elemental chemical analysis, dynamic light scattering (DLS), zeta (ζ)-potential and solid-state nuclear magnetic resonance (NMR). “In vial” LEVO release profiles and the in vitro antimicrobial effectiveness of the different released doses were investigated. The efficacy of the nanoantibiotic against a S. aureus biofilm was also determined, showing the practically total destruction of the biofilm due to the high penetration ability of the developed nanosystem. These findings open up promising expectations in the field of bone infection treatment.

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Amphiphilic Copolymer of Polyhedral Oligomeric Silsesquioxane (POSS) Methacrylate for Solid Dispersion of Paclitaxel

Materials ◽

10.3390/ma12071058 ◽

2019 ◽

Vol 12 (7) ◽

pp. 1058 ◽

Cited By ~ 2

Author(s):

Suchismita Chatterjee ◽

Tooru Ooya

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Aqueous Media ◽

Amorphous State ◽

Polyhedral Oligomeric Silsesquioxane ◽

Aqueous Solubility ◽

Polymer Mixtures ◽

Scanning Calorimetry ◽

New Formulation ◽

Oligomeric Silsesquioxane

Suitable polymers for the homogeneous formulation of drug/polymer mixtures should be selected to correct the structural and physicochemical nature with a rapid dissolution rate. This study aimed to evaluate a copolymer prepared by the radical polymerization of 2-methacryloyloxyethyl phosphorylcholine (MPC) and a polyhedral oligomeric silsesquioxane (POSS) methacrylate bearing an ethyl (C2H5) group (MPC-ran-C2H5-POSS) as a carrier for the solid formulation of paclitaxel (PTX). A single-phase homogeneous formulation of PTX with the mixture of the MPC-ran-C2H5-POSS and polyvinylpyrrolidone (PVP) was prepared by a solvent method. The formulation of MPC-ran-C2H5-POSS/PVP/PTX enhanced the dissolution rate and the dissolved amount (approximately 90% within 40 min) without precipitation. The X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) analysis confirmed the presence of PTX as an amorphous state. The amphiphilic nature of the MPC-ran-C2H5-POSS contributed to enhancing the aqueous solubility of PTX. The new formulation is applicable for solid dispersion technique via the supersaturation of PTX in an aqueous media.

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Artemether-Soluplus Hot-Melt Extrudate Solid Dispersion Systems for Solubility and Dissolution Rate Enhancement with Amorphous State Characteristics

Journal of Pharmaceutics ◽

10.1155/2013/151432 ◽

2013 ◽

Vol 2013 ◽

pp. 1-15 ◽

Cited By ~ 3

Author(s):

Ritesh A. Fule ◽

Tarique S. Meer ◽

Ajay R. Sav ◽

Purnima D. Amin

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Amorphous State ◽

Polymer Melt ◽

Aqueous Solubility ◽

Dissolution Profile ◽

Scanning Calorimetry ◽

Peg 400 ◽

Hot Melt

This work studied artemether (ARTM) solid dispersion (SD) formulation using mixture of polymer excipient Soluplus, PEG 400, Lutrol F127, and Lutrol F68 melts at temperatures lower than the melting point of ARTM using a laboratory-size, single-screw rotating batch extruder. The effects of three surfactants PEG 400, Lutrol F127, and Lutrol F68 and parameters like mixing temperature, screw rotating speed, and residence time were systematically studied. SEM, XRD, and FT-IR were employed to investigate the evolution of ARTM’s dissolution into the molten excipient. Differential scanning calorimetry (DSC) was used to quantitatively study the melting enthalpy evolution of the drug. The results showed that the dissolution rate increased with increasing the ratio of polymer and surfactant to that of drug. It was concluded that the dissolution of the drug in the polymer melt is a convective diffusion process and that laminar distributive mixing can significantly enhance the dissolution rate. The aqueous solubility and dissolution rate of prepared solid dispersion were significantly enhanced. In vitro antimalarial studies revealed marked improvement in IC50 values. Thus hot-melt extrusion (HME) is a promising technology for improving solubility and dissolution profile of ARTM.

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Solubility Enhancement of Poorly Soluble Drug Simvastatin by Solid Dispersion Technique

Research in Pharmacy and Health Sciences ◽

10.32463/rphs.2016.v02i02.16 ◽

2016 ◽

Vol 2 (2) ◽

pp. 91-95

Author(s):

Neelima Rani T ◽

Pavani A ◽

Sobhita Rani P ◽

Srilakshmi N

Keyword(s):

Dissolution Rate ◽

Drug Carrier ◽

Solid Dispersions ◽

Aqueous Solubility ◽

Onset Of Action ◽

Kneading Method ◽

Wetting Property ◽

Poorly Soluble ◽

Dispersion Technique ◽

Low Solubility

This study aims to formulate solid dispersions (SDs) of Simvastatin (SIM) to improve the aqueous solubility, dissolution rate and to facilitate faster onset of action. Simvastatin is a BCS class II drug having low solubility & therefore low oral bioavailability. In the present study, SDs of simvastatin different drug-carrier ratios were prepared by kneading method. The results showed that simvastatin solubility & dissolution rate enhanced with polymer SSG in the ratio 1:7 due to increase in wetting property or possibly may be due to change in crystallinity of the drug.

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