Melatonin-loaded lecithin/chitosan nanoparticles: physicochemical characterisation and permeability through Caco-2 cell monolayers.

Abstract:

:In this study, the potential of lecithin/chitosan nanoparticles (NPs) as a mucoadhesive colloidal nanosystem for transmucosal delivery of melatonin was investigated. The size, zeta potential and melatonin loading of the lecithin/chitosan NPs were investigated as a function of lecithin type (Lipoid S45, S75 and S100) and chitosan content in the preparation. The NPs were characterised by mean diameter and zeta potential ranging between 121.6 and 347.5 nm, and 7.5 and 32.7 mV, respectively, and increasing with lecithin-negative charge and chitosan content in the preparation. Melatonin loadings were up to 7.1%. All NPs were characterised by prolonged release profiles with an initial burst (approximately 25%), followed by a slow release phase. Approximately 60-70% of melatonin was released in 4h. The permeability of melatonin was investigated using Caco-2 cells as an in vitro model of the epithelial barrier. Melatonin permeability from an NP suspension prepared with Lipoid S45 lecithin and a lecithin-to-chitosan weight ratio (L/C) of 20:1 (sample C2) was significantly improved compared to the permeability of melatonin from the solution (P<0.001) and from all other NPs investigated (P<0.05). The results obtained by the cell viability studies (MTT and LDH leakage assays) showed that C2 NP suspension did not induce plasma membrane damage or decrease cell viability and could be safely applied to Caco-2 cells in the concentration range tested (<400 microg/ml).

journal_name

Int J Pharm

authors

Hafner A,Lovrić J,Voinovich D,Filipović-Grcić J

doi

10.1016/j.ijpharm.2009.07.001

subject

Has Abstract

pub_date

2009-11-03 00:00:00

pages

205-13

issue

2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(09)00454-2

journal_volume

381

pub_type

杂志文章
  • Production and evaluation of size reduced grades of microcrystalline cellulose.

    abstract::Size reduction of microcrystalline cellulose (MCC, Avicel PH-101) powder by ball milling was poorly effective, particularly in the presence of sodium lauryl sulphate (SLS), which tended to form a protective foam. Ultrasonic homogenisation of an aqueous suspension more readily produced ultra-fine MCC, even in the prese...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(00)00652-9

    authors: Levis SR,Deasy PB

    更新日期:2001-02-01 00:00:00

  • Controlled dual release of basic fibroblast growth factor and indomethacin from heparin-conjugated polymeric micelle.

    abstract::This work describes the development of heparinized polymeric micelle as a novel injectable carrier for the dual drug delivery that can simultaneously release basic fibroblast growth factor (bFGF) and indomethacin (IMC), which can promote the regeneration of damaged tissue and prevent the inflammatory response after im...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.06.025

    authors: Lee JS,Bae JW,Joung YK,Lee SJ,Han DK,Park KD

    更新日期:2008-01-04 00:00:00

  • Influence of the unloading conditions on capping and lamination: Study on a compaction simulator.

    abstract::Capping and lamination are classical industrial issues that can be challenging during the scale up of solid dosage forms. Previous publications showed that changing the unloading conditions (triaxial decompression, loaded ejection) made it possible to mitigate capping. In the present study, a systematic study of the e...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.118468

    authors: Mazel V,Desbois L,Tchoreloff P

    更新日期:2019-08-15 00:00:00

  • Improvement of cellular uptake, in vitro antitumor activity and sustained release profile with increased bioavailability from a nanoemulsion platform.

    abstract::Paclitaxel, a potential anticancer agent against solid tumors has been restricted from its oral use due to poor water solubility as well as Pgp efflux property. The present study was aimed to improve the oral bioavailability of paclitaxel through development of (o/w) nanoemulsion consisting of Capryol 90 as internal p...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.10.055

    authors: Choudhury H,Gorain B,Karmakar S,Biswas E,Dey G,Barik R,Mandal M,Pal TK

    更新日期:2014-01-02 00:00:00

  • Hydrophobically modified inulin as an amphiphilic carbohydrate polymer for micellar delivery of paclitaxel for intravenous route.

    abstract::Micellization offers several advantages for the delivery of water insoluble drugs including a nanoparticulate 'core-shell' delivery system for drug targeting. Recently, hydrophobically modified polysaccharides (HMPs) are gaining recognition as micelle forming polymers to encapsulate hydrophobic drugs. In this manuscri...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.01.005

    authors: Muley P,Kumar S,El Kourati F,Kesharwani SS,Tummala H

    更新日期:2016-03-16 00:00:00

  • Determination of acetaminophen's solubility in poly(ethylene oxide) by rheological, thermal and microscopic methods.

    abstract::A drug's solubility in a polymeric excipient is an important parameter that dictates the process window of hot-melt extrusion (HME) and product stability during storage. However, it is rather challenging to experimentally determine the solubility and there is very few published work in this field. In this study, the s...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.10.026

    authors: Yang M,Wang P,Suwardie H,Gogos C

    更新日期:2011-01-17 00:00:00

  • Characterisation of solid dispersions of paracetamol and EUDRAGIT E prepared by hot-melt extrusion using thermal, microthermal and spectroscopic analysis.

    abstract::Hot-melt extrusion has attracted considerable interest within the pharmaceutical industry. However, there remains some uncertainty as to how to characterise the physical structure of the extruded systems, particularly in terms of identifying the nature of the drug dispersion within the polymer. The aim of the study wa...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.11.048

    authors: Qi S,Gryczke A,Belton P,Craig DQ

    更新日期:2008-04-16 00:00:00

  • Design of nonionic micelle-laden polysaccharide hydrogels for controlled delivery of hydrophobic drugs.

    abstract::The incorporation of micelle self-assembly in hydrogels has been used to produce self-healing materials, materials with tunable mechanical properties, and hydrophilic or hydrophobic drug delivery systems. However, little is known about the connection among formulation - structure - properties (particularly transport) ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.04.062

    authors: Munoz SZ,Zhadan R,Acosta E

    更新日期:2017-06-30 00:00:00

  • Polymer sutures for simultaneous wound healing and drug delivery - A review.

    abstract::Drug delivery using suitable polymeric devices has gathered momentum in the recent years due to their remarkable properties. The versatility of polymeric materials makes them reliable candidates for site targeted drug release. Among them biodegradable sutures has received considerable attention because they offer grea...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2017.03.041

    authors: Joseph B,George A,Gopi S,Kalarikkal N,Thomas S

    更新日期:2017-05-30 00:00:00

  • Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG.

    abstract::The aim of this study was to design a controlled release vehicle for insulin to preserve its stability and biological activity during fabrication and release. A modified, double emulsion, solvent evaporation, technique using homogenisation force optimised entrapment efficiency of insulin into biodegradable nanoparticl...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.12.063

    authors: Haggag Y,Abdel-Wahab Y,Ojo O,Osman M,El-Gizawy S,El-Tanani M,Faheem A,McCarron P

    更新日期:2016-02-29 00:00:00

  • Carrageenan-based physically crosslinked injectable hydrogel for wound healing and tissue repairing applications.

    abstract::In this study, a novel injectable hydrogel based on iota and kappa carrageenan, locust bean gum and gelatin was prepared for wound healing and tissue repairing applications. This injectable hydrogel was obtained via physical crosslinking. FTIR analysis confirmed the physical interaction between the biopolymeric compon...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119828

    authors: Pettinelli N,Rodríguez-Llamazares S,Bouza R,Barral L,Feijoo-Bandín S,Lago F

    更新日期:2020-08-29 00:00:00

  • Characterization of nifedipine microparticles prepared by hot air coating technique.

    abstract::In the present work, the Hot Air Coating (HAC) technique was used to prepare microparticulate systems containing nifedipine. Binary mixtures constituting of nifedipine and cetearyl alcohol (CA) in different proportions (30:70, 50:50, 70:30) were studied: they were homogenized by mixing or milling before spray treatmen...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2005.01.010

    authors: Giovannelli L,Bellomi S,Pattarino F,Albertini B

    更新日期:2005-04-11 00:00:00

  • Knowledge management in secondary pharmaceutical manufacturing by mining of data historians-A proof-of-concept study.

    abstract::In this proof-of-concept study, a methodology is proposed to systematically analyze large data historians of secondary pharmaceutical manufacturing systems using data mining techniques. The objective is to develop an approach enabling to automatically retrieve operation-relevant information that can assist the managem...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.03.035

    authors: Meneghetti N,Facco P,Bezzo F,Himawan C,Zomer S,Barolo M

    更新日期:2016-05-30 00:00:00

  • Application of spherical silicate to prepare solid dispersion dosage forms with aqueous polymers.

    abstract::The objective of this study is to prepare and characterize solid dispersions of nifedipine (NP) using porous spherical silicate micro beads (MB) that were approximately 100 μm in diameter with vinylpyrrolidone/vinyl acetate copolymer (PVP/VA) and a Wurster-type fluidized bed granulator. Compared with previously report...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.07.037

    authors: Nagane K,Kimura S,Ukai K,Takahashi C,Ogawa N,Yamamoto H

    更新日期:2015-09-30 00:00:00

  • The breakage behaviour of Aspirin under quasi-static indentation and single particle impact loading: effect of crystallographic anisotropy.

    abstract::The influence of crystallographic structural anisotropy on the breakage behaviour of Aspirin under impact loading is highlighted. Under both quasi-static testing conditions, using nano-indentation, and dynamic impact tests, Aspirin demonstrates clear anisotropy in its slip and fracture behaviour. During nano-indentati...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.03.039

    authors: Olusanmi D,Roberts KJ,Ghadiri M,Ding Y

    更新日期:2011-06-15 00:00:00

  • Effect of diclofenac and glycol intercalation on structural assembly of phospholipid lamellar vesicles.

    abstract::The aim of the current study was to improve the knowledge of drug-glycol-phospholipid-interactions and their effects in lamellar vesicle suitability as drug delivery systems. Liposomes were prepared using hydrogenated soy phosphatidylcholine (P90H, 60 mg/ml) and diclofenac sodium salt at two concentrations (5-10 mg/ml...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.08.034

    authors: Castangia I,Manca ML,Matricardi P,Sinico C,Lampis S,Fernàndez-Busquets X,Fadda AM,Manconi M

    更新日期:2013-11-01 00:00:00

  • Downregulation of survivin expression and enhanced chemosensitivity of MCF-7 cells to adriamycin by PDMAE/survivin shRNA complex nanoparticles.

    abstract::Gene silencing mediated by RNA interference (RNAi) presents a promising strategy for gene therapy. The aim of this work is to evaluate a new gene delivery system for downregulation of survivin expression and enhanced chemosensitivity of MCF-7 cells to adriamycin (ADR). A new cationic poly(2-dimethylaminoethylamine/2-(...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.11.047

    authors: Yang Y,Gao Y,Chen L,Huang Y,Li Y

    更新日期:2011-02-28 00:00:00

  • In vivo distribution of arsonoliposomes: effect of vesicle lipid composition.

    abstract::Sonicated arsonoliposomes were prepared using arsonolipid with palmitic acid acyl chain (C16), mixed with 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC-based), and cholesterol (Chol) with a molar ratio C16/DSPC/Chol 8:12:10. PEG-lipid (1,2-distearoyl-sn-glycero-3-phosphoethanolamine conjugated to polyethylenoglycol...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.06.048

    authors: Zagana P,Haikou M,Klepetsanis P,Giannopoulou E,Ioannou PV,Antimisiaris SG

    更新日期:2008-01-22 00:00:00

  • Oral insulin delivery in rats by nanoparticles prepared with non-toxic solvents.

    abstract::Nanoparticles (NPs) have shown a certain potential to overcome the drawbacks of oral peptide delivery in the gastrointestinal tract such as low peptide stability and permeability. The preparation of insulin loaded NPs was carried out with Eudragit RL or RS dissolved in different non-toxic polyethylene glycol (PEG) der...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.01.017

    authors: Viehof A,Javot L,Béduneau A,Pellequer Y,Lamprecht A

    更新日期:2013-02-25 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

  • Optimisation of floating matrix tablets and evaluation of their gastric residence time.

    abstract::The present investigation concerns the development of the floating matrix tablets, which after oral administration are designed to prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. The importance of the composition optimisation, the technological p...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(99)00378-6

    authors: Baumgartner S,Kristl J,Vrecer F,Vodopivec P,Zorko B

    更新日期:2000-02-15 00:00:00

  • Design and physicochemical stability studies of paediatric oral formulations of sildenafil.

    abstract::Personalized medicine is a challenging research area in paediatric treatments. Elaborating new paediatric formulations when no commercial forms are available is a common practice in pharmacy laboratories; among these, oral liquid formulations are the most common. But due to the lack of specialized equipment, frequentl...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.11.006

    authors: Provenza N,Calpena AC,Mallandrich M,Halbaut L,Clares B

    更新日期:2014-01-02 00:00:00

  • Validation of a continuous granulation process using a twin-screw extruder.

    abstract::Using twin-screw granulation as particle size enlargement technique, the effect of modifying the screw configuration (number of mixing zones, configuration of kneading block) on granule quality, tablet properties and mixing efficiency was investigated. The amount of oversized agglomerates and yield was significantly i...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.01.012

    authors: Van Melkebeke B,Vervaet C,Remon JP

    更新日期:2008-05-22 00:00:00

  • Controlled-release triple anti-inflammatory therapy based on novel gastroretentive sponges: characterization and magnetic resonance imaging in healthy volunteers.

    abstract::The current work aimed to develop novel composite sponges of chitosan (CH)-chondroitin sulfate (CS) as a low-density gastroretentive delivery system for lornoxicam (LOR). This triple anti-inflammatory therapy-loaded matrices are expected to expand and float upon contact with gastric fluids for prolonged times. CH and ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.06.013

    authors: Tadros MI,Fahmy RH

    更新日期:2014-09-10 00:00:00

  • Enhanced transdermal delivery of low molecular weight heparin by barrier perturbation.

    abstract::The purpose of this work was to investigate the in vitro transdermal delivery of low molecular weight heparin (LMWH). Hairless rat skin was mounted on Franz diffusion cells and treated with various enhancement strategies. Passive flux was essentially zero and remained low even after iontophoresis (0.065 U cm(-2) h(-1)...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.08.028

    authors: Lanke SS,Kolli CS,Strom JG,Banga AK

    更新日期:2009-01-05 00:00:00

  • Contribution of TRPV1 and multidrug resistance proteins in the permeation of capsaicin across different intestinal regions.

    abstract:OBJECTIVE:The aim of the study was to observe the characteristic of permeation of capsaicin across jejunum, ileum and colon in the rat, and to investigate the role of transient receptor potential cation channel (TRPV1). The interaction of capsaicin with P-glycoprotein (P-gp), multidrug resistance-associated protein 2 (...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.02.007

    authors: Duan L,Yan Y,Sun Y,Zhao B,Hu W,Li G

    更新日期:2013-03-10 00:00:00

  • A systematic study of captopril-loaded polyester fiber mats prepared by electrospinning.

    abstract::In this study, drug-loaded nanofibers were prepared by electrospinning captopril (CPL) with aliphatic biodegradable polyesters. Poly(L-lactic acid) (PLLA), poly(lactic-co-glycolic acid) (PLGA), and poly(lactic-co-ε-caprolactone) (PLCL) were used as filament-forming matrix polymers, and the concentration of CPL in each...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.09.055

    authors: Zhang H,Lou S,Williams GR,Branford-White C,Nie H,Quan J,Zhu LM

    更新日期:2012-12-15 00:00:00

  • Fluid bed agglomeration with a narrow droplet size distribution.

    abstract::In the fluid bed agglomeration processes liquid distribution influences the agglomerate growth. We developed a new nozzle that produces uniform droplets, which allows droplets to be easily controlled in size independently of liquid- and airflow of the nozzle. It was found that the spray rate and the mixing in the spra...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(99)00329-4

    authors: Schaafsma SH,Vonk P,Kossen NW

    更新日期:2000-01-05 00:00:00

  • Improved oral bioavailability and anticancer efficacy on breast cancer of paclitaxel via Novel Soluplus(®)-Solutol(®) HS15 binary mixed micelles system.

    abstract::The aim of this study was to develop a novel drug delivery system using two biocompatible copolymers of Solutol(®)HS15 and Soluplus(®) to improve solubility, oral bioavailability and anticancer activity of paclitaxel (PTX). The PTX-loaded mixed micelles (PTX-M) were prepared by ethanol thin-film hydration method. The ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.08.045

    authors: Hou J,Sun E,Sun C,Wang J,Yang L,Jia XB,Zhang ZH

    更新日期:2016-10-15 00:00:00

  • Pharmacokinetics of Gastrodin in rat plasma and CSF after i.n. and i.v.

    abstract::The pharmacokinetic behavior of Gastrodin in rat plasma and cerebrospinal fluid (CSF) after intranasal and intravenous administration (50mg kg(-1)) was investigated. Intranasal administration of Gastrodin provided a comparable AUC in CSF compared with the intravenous administration. But Gastrodin level in plasma was v...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.03.041

    authors: Wang Q,Chen G,Zeng S

    更新日期:2007-08-16 00:00:00