Preparation and optimization of fisetin loaded glycerol based soft nanovesicles by Box-Behnken design.

Abstract:

:The present study focused on the development and optimization of glycerosomes for dermal delivery of fisetin. The fisetin loaded glycerosomes formulation was optimized by Box-Behnken design. The independent variables were the lipoid S 100, glycerol, and sonication time, whereas the dependent variables were the vesicles size, entrapment efficiency, and flux. The mechanism of skin penetration of fisetin loaded glycerosomes formulation was determined by the DSC and FTIR studies. Confocal scanning microscopy was used to detect the penetration ability of glycerosomes. The optimized fisetin loaded glycerosomes formulation was converted into a Carbopol® gel matrix, and the latter was analyzed for various parameters. The optimized formulation of glycerosomes presented vesicles size, entrapment efficiency and flux of 138.8 ± 4.09 nm, 86.41 ± 2.95% and 5.04 ± 0.17 µg/cm2/h, respectively. The transmission electron microscopy of optimized fisetin loaded formulation revealed the spherical and sealed structure of glycerosomes vesicles. The confocal study confirmed that the Rhodamine B incorporated glycerosomes penetrated up to deeper layers of skin. The DSC and FTIR studies revealed that the hydration of skin layers and skin lipid fluidization could be the penetration mechanism of fisetin glycerosomes formulation. The optimized fisetin loaded glycerosomes gel formulation presented a flux of 4.24 ± 0.14 μg/cm2/h, and exhibited zero-order release kinetics. The texture analysis of fisetin glycerosomes gel displayed a sufficient hardness, consistency, cohesiveness, and index of viscosity. It was concluded that the prepared fisetin loaded glycerosomes gel was suitable for the dermal application.

journal_name

Int J Pharm

authors

Moolakkadath T,Aqil M,Ahad A,Imam SS,Praveen A,Sultana Y,Mujeeb M

doi

10.1016/j.ijpharm.2020.119125

subject

Has Abstract

pub_date

2020-03-30 00:00:00

pages

119125

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(20)30109-5

journal_volume

578

pub_type

杂志文章
  • Fabrication of nanopatterned PLGA films of curcumin and TPGS for skin cancer.

    abstract::Squamous cell carcinoma treatment has limited therapeutic options and the incidence rate is increasing recently. In the present investigation, we developed poly(lactic-co-glycolic acid) (PLGA) nanopatterned films (NPFs) through poly dimethyl siloxane (PDMS) cast molding technique and explored its therapeutic efficacy ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119100

    authors: Malathi S,Pavithra PS,Sridevi S,Verma RS

    更新日期:2020-03-30 00:00:00

  • An improved method for the characterization of supersaturation and precipitation of poorly soluble drugs using pulsatile microdialysis (PMD).

    abstract::In current pharmaceutical drug discovery, most candidates are poorly soluble in water, which can result in poor bioavailability. To overcome this problem, formulations that create supersaturation of the drug are a well-studied alternative. Characterizing the dissolution from these systems is challenging because conven...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.04.012

    authors: Shah KB,Patel PG,Khairuzzaman A,Bellantone RA

    更新日期:2014-07-01 00:00:00

  • A tunable extruded 3D printing platform using thermo-sensitive pastes.

    abstract::Extruded 3D printing is emerging as an attractive fabrication technology in the field of personalized oral medicines. The objective of this study was to develop a tunable extruded 3D printing platform based on thermo-sensitive gelatin pastes to meet the needs of achieving different drug release characteristics with fl...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119360

    authors: Yang Y,Wang X,Lin X,Xie L,Ivone R,Shen J,Yang G

    更新日期:2020-06-15 00:00:00

  • Formation of multicellular tumor spheroids induced by cyclic RGD-peptides and use for anticancer drug testing in vitro.

    abstract::Development of novel anticancer formulations is a priority challenge in biomedicine. However, in vitro models based on monolayer cultures (2D) which are currently used for cytotoxicity tests leave much to be desired. More and more attention is focusing on 3D in vitro systems which can better mimic solid tumors. The ai...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.04.005

    authors: Akasov R,Zaytseva-Zotova D,Burov S,Leko M,Dontenwill M,Chiper M,Vandamme T,Markvicheva E

    更新日期:2016-06-15 00:00:00

  • Synthesis, characterization, in vitro and in vivo evaluation of PEGylated oridonin conjugates.

    abstract::Oridonin (ORI), a diterpenoid compound with promising antitumor activity, was proved to possess potent antileukemia efficacies in vitro and in vivo recently. However, the development and application of ORI was limited by its poor solubility and rapid plasma clearance. The purpose of this study was to solve these probl...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.08.014

    authors: Shen J,Zhang D,Zhao Z,Jia L,Zheng D,Liu G,Hao L,Zhang Q,Tian X,Li C,Guo H

    更新日期:2013-11-01 00:00:00

  • Sustained intrathecal therapeutic protein delivery using genetically transduced tissue implants in a freely moving rat model.

    abstract::Systemic delivery of therapeutic proteins to the central nervous system (CNS) is challenging because of the blood-brain barrier restrictions. Direct intrathecal delivery is possible but does not produce stable concentrations. We are proposing an alternative approach for localized delivery into the CNS based on the Tra...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.10.002

    authors: Aronson JP,Katnani HA,Pomerantseva I,Shapir N,Tse H,Miari R,Goltsman H,Mwizerwa O,Neville CM,Neil GA,Eskandar EN,Sundback CA

    更新日期:2017-12-20 00:00:00

  • Novel Curcumin loaded nanoparticles engineered for Blood-Brain Barrier crossing and able to disrupt Abeta aggregates.

    abstract::The formation of extracellular aggregates built up by deposits of β-amyloid (Aβ) is a hallmark of Alzheimer's disease (AD). Curcumin has been reported to display anti-amyloidogenic activity, not only by inhibiting the formation of new Aβ aggregates, but also by disaggregating existing ones. However, the uptake of Curc...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.05.015

    authors: Barbara R,Belletti D,Pederzoli F,Masoni M,Keller J,Ballestrazzi A,Vandelli MA,Tosi G,Grabrucker AM

    更新日期:2017-06-30 00:00:00

  • Biocompatible, biodegradable and sterically stabilized phospholipid nanomicelles improve cryopreservation of oral keratinocytes: a preliminary investigation.

    abstract::In this proof-of principle study, we determined whether biocompatible, biodegradable and sterically stabilized phospholipid nanomicelles (SSNMs) improve viability and membrane integrity of cryopreserved oral keratinocytes. Cultured chemically transformed hamster oral keratinocytes were frozen gradually with and stored...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.02.002

    authors: Rubinstein I,Onyüksel H

    更新日期:2007-06-29 00:00:00

  • Assessment of disorder in crystalline powders--a review of analytical techniques and their application.

    abstract::The need to be able to measure amorphous contents in crystalline powders is now recognised. In this review, calorimetric and gravimetric methods are reviewed in a way that should alert workers in the field to the theoretical, and practical considerations which are important to understanding how best to study crystalli...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/s0378-5173(98)00335-4

    authors: Buckton G,Darcy P

    更新日期:1999-03-15 00:00:00

  • Evaluation of the effect of rifampicin on the biophysical properties of the membranes: significance for therapeutic and side effects.

    abstract::This work aims to study the biophysical interactions of rifampicin (RIF) with three-dimensional macrophage membrane models, under environments with physiological and pathological relevance. The interaction of RIF with liposomes formed by 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) in different pH values (i.e., ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.03.005

    authors: Pinheiro M,Pisco S,Silva AS,Nunes C,Reis S

    更新日期:2014-05-15 00:00:00

  • ESR studies on the influence of physiological dissolution and digestion media on the lipid phase characteristics of SEDDS and SEDDS pellets.

    abstract::The aim of the current study is the evaluation of a recently optimized SEDDS, composed of Solutol HS15 and medium chain glycerides, and self-emulsifying pellets by means of ESR. Tempol-benzoate (TB)-loaded SEDDS were produced and electron spin resonance (ESR) spectroscopy was used to evaluate the diluted self-emulsify...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.09.014

    authors: Abdalla A,Mäder K

    更新日期:2009-02-09 00:00:00

  • An in vitro kinetic method for detection of precipitation of poorly soluble drugs.

    abstract::A simple in vitro method for the detection of precipitation using 96-well microplates and a SpectraMax Plus microtiter plate reader has been developed and described. The method requires only small amount of drug and is, therefore, potentially applicable in early pre-formulation. The method is based on opacity changes ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2005.08.012

    authors: Wu Z,Tucker IG,Razzak M,Medlicott NJ

    更新日期:2005-11-04 00:00:00

  • Swallowing dysfunction and dysphagia is an unrecognized challenge for oral drug therapy.

    abstract::There is evidence that swallowing issues and dysphagia are an increasing problem of the aging population in the coming decades that is affecting oral medication administration. There is a variety of clinical expressions of swallowing dysfunction caused by aging, acute or chronic disease conditions, decline in physiolo...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2012.04.022

    authors: Stegemann S,Gosch M,Breitkreutz J

    更新日期:2012-07-01 00:00:00

  • Effect of aqueous solubility of grafted moiety on the physicochemical properties of poly(d,l-lactide) (PLA) based nanoparticles.

    abstract::In order to evaluate the solubility effect of grafted moiety on the physicochemical properties of poly(d,l-lactide) (PLA) based nanoparticles (NPs), two materials of completely different aqueous solubility, polyethylene glycol (PEG) and palmitic acid were grafted on PLA backbone at nearly the same grafting density, 2....

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2009.12.059

    authors: Essa S,Rabanel JM,Hildgen P

    更新日期:2010-03-30 00:00:00

  • Interaction of cationic partial dendrimers with charged and neutral liposomes.

    abstract::Amphipathic partial dendrimers having three lipidic (C(14)) chains coupled to dendritic lysine head groups with eight, 16 or 32 free terminal amino groups have been synthesised by solid-phase peptide synthesis. Liposomes were prepared with positive, negative and neutral charge using the dehydration-rehydration method ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(00)00635-9

    authors: Purohit G,Sakthivel T,Florence AT

    更新日期:2001-02-19 00:00:00

  • Carrier-based dry powder inhalation: Impact of carrier modification on capsule filling processability and in vitro aerodynamic performance.

    abstract::This study aims to investigate the effect of carrier characteristics and dosator capsule filling operation on the in vitro deposition of mixtures containing salbutamol sulphate (SS) and lactose and mannitol as model carrier materials. The carrier surfaces of lactose and mannitol were modified via wet decantation. The ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.06.044

    authors: Faulhammer E,Wahl V,Zellnitz S,Khinast JG,Paudel A

    更新日期:2015-08-01 00:00:00

  • Glucan particles as suitable carriers for the natural anti-inflammatory compounds curcumin and diplacone - Evaluation in an ex vivo model.

    abstract::Natural compounds offer a wide spectrum of potential active substances, but often they have a poor bioavailability. To increase the bioavailability and bioactivity of the natural anti-inflammatory molecules curcumin and diplacone, we used glucan particles (GPs), hollow shells from Saccharomyces cerevisiae composed mai...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119318

    authors: Rotrekl D,Devriendt B,Cox E,Kavanová L,Faldyna M,Šalamúnová P,Baďo Z,Prokopec V,Štěpánek F,Hanuš J,Hošek J

    更新日期:2020-05-30 00:00:00

  • Dissolution performance of binary amorphous drug combinations--Impact of a second drug on the maximum achievable supersaturation.

    abstract::An increased number of amorphous formulations of poorly water soluble drugs are being introduced into the market due to their higher transient solubility and thus faster absorption and higher bioavailability. While most amorphous drug products contain a single drug substance, there is a growing trend towards co-formul...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.10.026

    authors: Trasi NS,Taylor LS

    更新日期:2015-12-30 00:00:00

  • Stability of luciferase plasmid entrapped in cationic bilayer vesicles.

    abstract::Characteristics and physical stability of luciferase plasmid (pLuc) entrapped in cationic bilayer vesicles prepared from various molar ratios of amphiphiles (DPPC, Tween61 or Span60), cholesterol (Chol) and cationic charge lipid (DDAB) were investigated. The cationic liposomes were composed of DPPC/Chol/DDAB in the mo...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.01.001

    authors: Manosroi A,Thathang K,Werner RG,Schubert R,Manosroi J

    更新日期:2008-05-22 00:00:00

  • Predicting the gastrointestinal behaviour of modified-release products: utility of a novel dynamic dissolution test apparatus involving the use of bicarbonate buffers.

    abstract::The establishment of physiologically relevant in vitro-in vivo correlations (IV-IVCs) is key for any biorelevant dissolution test. Historically, bicarbonate buffers have produced better correlations than compendial phosphate buffered media, though such tests are usually performed at a constant pH experiment, overlooki...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.09.003

    authors: Merchant HA,Goyanes A,Parashar N,Basit AW

    更新日期:2014-11-20 00:00:00

  • Preparation, characterization and in vitro release study of a glutathione-dependent polymeric prodrug Cis-3-(9H-purin-6-ylthio)-acrylic acid-graft-carboxymethyl chitosan.

    abstract::In this work, an amphiphilic polymeric prodrug Cis-3-(9H-purin-6-ylthio)-acrylic acid-graft-carboxymethyl chitosan (PTA-g-CMCS) was designed and synthesized. In aqueous solution, this grafted polymer can self-assemble into spherical micelles with a size ranging from 104 to 285 nm and zeta potential ranging from -12.3 ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.06.043

    authors: Gong XY,Yin YH,Huang ZJ,Lu B,Xu PH,Zheng H,Xiong FL,Xu HX,Xiong X,Gu XB

    更新日期:2012-10-15 00:00:00

  • Chitosan and its derivatives: potential excipients for peroral peptide delivery systems.

    abstract::In the 1990s chitosan turned out to be a useful excipient in various pharmaceutical formulations. By modifications of the primary amino group at the 2-position of this poly(beta1-->4 D-glucosamine), the features of chitosan can even be optimised according to a given task in drug delivery systems. For peroral peptide d...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/s0378-5173(99)00365-8

    authors: Bernkop-Schnürch A

    更新日期:2000-01-20 00:00:00

  • Pluripotent stem cells as new drugs? The example of Parkinson's disease.

    abstract::Cell replacement therapy is a widely discussed novel concept of medical treatment. The increased knowledge in the stem cell field, particularly pluripotent stem cells, potentially provides powerful tools for this therapeutic concept. A large number of disease characterized by the loss of functional cells are potential...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2009.03.003

    authors: Preynat-Seauve O,Burkhard PR,Villard J,Zingg W,Ginovart N,Feki A,Dubois-Dauphin M,Hurst SA,Mauron A,Jaconi M,Krause KH

    更新日期:2009-11-03 00:00:00

  • Lectin-mediated drug delivery: binding and uptake of BSA-WGA conjugates using the Caco-2 model.

    abstract::To examine whether the dietary lectin wheat germ agglutinin (WGA) can facilitate binding and uptake of protein drugs due to its cytoadhesive and cytoinvasive properties, conjugates were prepared by covalent coupling of fluorescein-labeled bovine serum albumin (F-BSA) to WGA using divinylsulfone for crosslinking. Incre...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00049-2

    authors: Gabor F,Schwarzbauer A,Wirth M

    更新日期:2002-04-26 00:00:00

  • Polymeric micelles for the solubilization and delivery of STAT3 inhibitor cucurbitacins in solid tumors.

    abstract::Poly(ethylene oxide)-block-poly(epsilon-caprolactone) (PEO-b-PCL) and newly developed poly(ethylene oxide)-block-poly(alpha-benzyl carboxylate epsilon-caprolactone) (PEO-b-PBCL) micelles were evaluated for the solubilization and delivery of cucurbitacin I and B, poorly water soluble inhibitors of signal transducer and...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.06.032

    authors: Molavi O,Ma Z,Mahmud A,Alshamsan A,Samuel J,Lai R,Kwon GS,Lavasanifar A

    更新日期:2008-01-22 00:00:00

  • Wheat germ agglutinin-grafted lipid nanoparticles: preparation and in vitro evaluation of the association with Caco-2 monolayers.

    abstract::A bioadhesive drug delivery system, wheat germ agglutinin (WGA)-grafted lipid nanoparticles, was developed for the oral delivery of bufalin (a hydrophobic active component extracted from the traditional Chinese medicine Chan'su). The lipid nanoparticles associated with poly(vinyl alcohol) (PVA) were prepared by high-p...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.06.030

    authors: Liu Y,Wang P,Sun C,Feng N,Zhou W,Yang Y,Tan R,Chen Z,Wu S,Zhao J

    更新日期:2010-09-15 00:00:00

  • Ciprofloxacin nanocrystals liposomal powders for controlled drug release via inhalation.

    abstract::This study was conducted to evaluate the feasibility of developing inhalable dry powders of liposomal encapsulated ciprofloxacin nanocrystals (LECN) for controlled drug release. Dry powders of LECN were produced by freeze-thaw followed by spray drying. The formulations contained sucrose as a lyoprotectant in different...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.05.068

    authors: Khatib I,Khanal D,Ruan J,Cipolla D,Dayton F,Blanchard JD,Chan HK

    更新日期:2019-07-20 00:00:00

  • Oral sustained delivery of ambroxol from in situ-gelling pectin formulations.

    abstract::Gels formed in situ following oral administration of dilute aqueous solutions of pectin (1.0 and 1.5%, w/v) to rats were evaluated as vehicles for the sustained release of the expectorant drug ambroxol hydrochloride. The solutions contained calcium ions in complexed form, which on release in the acidic environment of ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2003.11.027

    authors: Kubo W,Miyazaki S,Dairaku M,Togashi M,Mikami R,Attwood D

    更新日期:2004-03-01 00:00:00

  • Study on jelly fig extract as a potential hydrophilic matrix for controlled drug delivery.

    abstract::The principal component of aqueous extract of jelly fig (Ficus awkeotsang Makino) seeds is a pectin-type polysaccharide, gelling even at room temperature without adding any sugars, acids or ions. The objective of this study was to evaluate jelly fig extract (JF) as a matrix base for sustained release tablets. Drug rel...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2004.08.023

    authors: Miyazaki Y,Yakou S,Takayama K

    更新日期:2004-12-09 00:00:00

  • Melt extrusion with poorly soluble drugs - An integrated review.

    abstract::Over the last few decades, hot melt extrusion (HME) has emerged as a successful technology for a broad spectrum of applications in the pharmaceutical industry. As indicated by multiple publications and patents, HME is mainly used for the enhancement of solubility and bioavailability of poorly soluble drugs. This revie...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2017.10.056

    authors: Repka MA,Bandari S,Kallakunta VR,Vo AQ,McFall H,Pimparade MB,Bhagurkar AM

    更新日期:2018-01-15 00:00:00