Modulating in vitro release and solubility of griseofulvin using functionalized mesoporous silica nanoparticles

Jambhrunkar, Siddharth; Qu, Zhi; Popat, Amirali; Karmakar, Surajit; Xu, Chun; Yu, Chengzhong

doi:10.1016/j.jcis.2014.08.019

Cited by 66 publications

(34 citation statements)

References 50 publications

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“…Despite this, efficacy of resveratrol in the clinical setting has been significantly restricted by poor physicochemical properties and limited success in creating therapeutic formulation using conventional drug delivery technologies. Therefore, a variety of nanoformulations have been proposed in order to circumvent its physicochemical hindrances with various advantages and challenges presented [10][11][12][13].…”

Section: Introductionmentioning

confidence: 99%

Enhancing delivery and cytotoxicity of resveratrol through a dual nanoencapsulation approach

Soo

Thakur

et al. 2016

Journal of Colloid and Interface Science

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107

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Despite the known anticancer potential of resveratrol, its clinical applications are often hindered by physicochemical limitations such as poor solubility and stability. The encapsulation of resveratrol in formulations such as polymeric nanoparticles and liposomes has shown limited success. This study aimed to develop and optimize a novel drug carrier by co-encapsulating pristine resveratrol alongside cyclodextrin-resveratrol inclusion complexes in the lipophilic and hydrophilic compartments of liposomes, respectively by using a novel dual carrier approach. The particle size, polydispersity index and zeta potential of the final formulation were 131±1.30nm, 0.089±0.005 and -2.64±0.51mV, respectively. Compared to free resveratrol and conventional liposomal formulations with drug release profile of 40-60%, our novel nanoformulations showed complete (100%) drug release in 24h. The formulation was stable for 14days at 4°C. We also studied the in vitro cytotoxicity of resveratrol encapsulated liposomes in HT-29 colon cancer cell lines. The cytotoxicity profile of our liposomes was observed to be dose dependent and enhanced in comparison to free resveratrol (in DMSO). Our study demonstrates that co-encapsulation of pristine resveratrol along with its cyclodextrin complex in liposomal formulations is a plausible option for the enhanced delivery of the hydrophobic chemotherapeutic agent.

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Section: Introductionmentioning

confidence: 99%

Enhancing delivery and cytotoxicity of resveratrol through a dual nanoencapsulation approach

Soo

Thakur

et al. 2016

Journal of Colloid and Interface Science

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107

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“…Some of the last reports in surface functionalization of MSP obtained from a TEOS sol-gel process are summarized in Table 2. It may be seen that most of the particles are type MCM-41 [78,79,[94][95][96][97][98][99], and few of them are from MCM-48 [100] or HMM [84]. All the others are catalogued as MSN [101][102][103][104][105][106][107][108], showing proof of mesostructured matrices with 2-4 nm average pore size, with exceptional sizes of 8 and 13 nm for HMM.…”

Section: Functionalized Mspmentioning

confidence: 93%

Colloidal and spherical mesoporous silica particles: synthesis and new technologies for delivery applications

Beltrán-Osuna

Perilla

2015

J Sol-Gel Sci Technol

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Continuous research in prominent fields such as biotechnology, biomedicine and nanopharmaceutics has brought the development of a widespread class of materials, and studies for mesoporous materials have been exponentially growing lately. The purpose of this review is to provide a useful guide for different materials, methods and configurations that have been reported in the last 5 years for the synthesis of spherical mesoporous silica particles (MSP), in the colloidal size range (1-1000 nm). MSP exhibit several limitations that must be overcome in order to enable their medical and clinical use. Surface modification of these particles will allow getting new promising characteristics of these materials, including better drug release control and biocompatibility improvement. These modified MSP could be potentially used in many biomedical applications, especially for drug delivery systems. Emphasis is made on the pore size, diameter and shape of the final particles since these parameters will establish key characteristics, i.e., drug delivery profile, loading capacity and efficiency. Graphical Abstract Spreading the use of mesoporous silica particles in biomedicine is possible by the improvement of its inner characteristics through surface modification. This may be done by chemical functionalization or by coating with macromolecular layers or brushes, thus creating novel responsive core-shell hybrid composites to be used as carriers for drug delivery applications.

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“…There are also publications on nanoparticles used to enhance the solubility, using mesoporous silica nanoparticles and a cyclodextrin nanoparticle combination. [18][19][20][21] Recently, FK506 prodrugs were synthesized to increase the solubility of FK506 through esterification using glucose or sialic acid (Figure 1). 22 The physicochemical characterizations on FK506 prodrugs (FK506-G or FK506-S) for the development of ocular formulation were carried out in this study.…”

Section: Introductionmentioning

confidence: 99%

Preformulation of FK506 Prodrugs for Improving Solubility

Jun

Kim³

et al. 2016

Bulletin Korean Chem Soc

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In order to improve water solubility of a lipophilic drug, tacrolimus (FK506), two prodrugs (FK506-G or FK506-S) such as FK506-M32-LS-G (FK506-G) and FK506-M32-LS-SL (FK506-S) were synthesized. Two prodrugs (FK506-G or FK506-S), including FK506, were characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), scanning electron microscopy (SEM), enzymatic kinetics, and cytotoxicity. A phase solubility test was conducted in distilled water, and the solubility of two prodrugs (FK506-G or FK506-S) was measured in various pH values for pH solubility profiles. Most interesting was that FK506-S showed the highest solubility, 866 μg/mL in water. In vitro enzymatic kinetics of two prodrugs (FK506-G or FK506-S) in human plasma was evaluated by measuring the decrease of FK506-G or FK506-S as well as the increase of FK506 by HPLC, and FK506-G or FK506-S was metabolized in 1 h in human plasma. Two prodrugs (FK506-G or FK506-S) including FK506 showed an IC 50 of 336.6 μg/mL for FK506, 337.9 μg/mL for FK506-G, or 480.1 μg/mL for FK506-S against a conjunctive cell line, Clone 1-5c-4 cells. Taken together, FK506-S could be the most optimal prodrug for aqueous preparations based on preformulation data.

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Modulating in vitro release and solubility of griseofulvin using functionalized mesoporous silica nanoparticles

Cited by 66 publications

References 50 publications

Enhancing delivery and cytotoxicity of resveratrol through a dual nanoencapsulation approach

Enhancing delivery and cytotoxicity of resveratrol through a dual nanoencapsulation approach

Colloidal and spherical mesoporous silica particles: synthesis and new technologies for delivery applications

Preformulation of FK506 Prodrugs for Improving Solubility

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