Thermosensitive glycol chitosan-based hydrogel as a topical ocular drug delivery system for enhanced ocular bioavailability.

Abstract:

:In the present study, we developed and evaluated an in situ gelling system based on hexanoyl glycol chitosan (H-GCS) for enhanced ocular bioavailability. An aqueous solution of H-GCS exhibited a typical sol-gel transition at 32 °C. The formed H-GCS hydrogel was characterized by rheology and scanning electron microscopy (SEM). H-GCS had minimal in vitro cytotoxicity against L-929 and HCEC cells over a concentration range of 0-0.8 mg/mL. Additionally, the H-GCS hydrogel exhibited good ocular tolerance and biocompatibility after a single instillation. Moreover, H-GCS hydrogel significantly prolonged the precorneal retention of fluorescein sodium compared with its aqueous solution. An in vivo pharmacokinetic study demonstrated that the levofloxacin-loaded H-GCS hydrogel could provide a significantly higher Cmax and AUC0-12h compared with the levofloxacin aqueous solution, thus increasing ocular bioavailability. Overall, the proposed H-GCS hydrogel acts as an in situ gelling system that might represent a promising vehicle for topical ocular drug delivery.

journal_name

Int J Pharm

authors

Shi H,Wang Y,Bao Z,Lin D,Liu H,Yu A,Lei L,Li X,Xu X

doi

10.1016/j.ijpharm.2019.118688

subject

Has Abstract

pub_date

2019-10-30 00:00:00

pages

118688

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(19)30733-1

journal_volume

570

pub_type

杂志文章
  • Synergistic enhancement of anticancer therapeutic efficacy of HPMA copolymer doxorubicin conjugates via combination of ligand modification and stimuli-response srategies.

    abstract::N-(2-Hydroxypropyl) methacrylamide (HPMA) copolymer has been extensively studied as drug carrier for tumor therapy. Due to the Enhanced Permeability and Retention (EPR) effect, HPMA copolymer drug conjugates are able to be passively accumulated in the tumor site. Currently, efficient uptake of this polymeric system by...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.12.018

    authors: Li L,Zhou M,Huang Y

    更新日期:2018-01-30 00:00:00

  • The influence of volatile solvents on transport across model membranes and human skin.

    abstract::Simple topical formulations which include volatile components, such as gels or sprays, are appealing from a cosmetic perspective. However, complex formulation effects may result from the use of volatile excipients in topical formulations, particularly when applied at clinically relevant doses (typically less than a fe...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.05.037

    authors: Oliveira G,Hadgraft J,Lane ME

    更新日期:2012-10-01 00:00:00

  • Synbiotic loaded chitosan-Ca-alginate microparticles reduces inflammation in the TNBS model of rat colitis.

    abstract::New therapeutic strategies against inflammatory bowel disease (IBD) consider the usage of probiotics, prebiotics and synbiotics as beneficial for the intestinal microbial balance. Limitations of such an approach are addressed into difference in survival, persistence, colonization and variable effects among different p...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.05.049

    authors: Ivanovska TP,Mladenovska K,Zhivikj Z,Pavlova MJ,Gjurovski I,Ristoski T,Petrushevska-Tozi L

    更新日期:2017-07-15 00:00:00

  • Physicochemical properties of macrogol ointment and emulsion ointment blend developed for regulation of water absorption.

    abstract::Pressure ulcers can form with excess pressure and shearing stress on skin tissue. Because pressure ulcer is often accompanies by exudates, selection of appropriate topical emulsion ointment is difficult. Blended ointments consisting of emulsion base and water-soluble base are clinically used for adjustment of wound mo...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.07.034

    authors: Noda Y,Watanabe K,Sanagawa A,Sobajima Y,Fujii S

    更新日期:2011-10-31 00:00:00

  • beta-carotene encapsulation in a mannitol matrix as affected by divalent cations and phosphate anion.

    abstract::The effects of addition of divalent cations and phosphate buffer on the degree of beta-carotene encapsulation in a mannitol matrix during freeze-drying were analyzed. The degradation rate of encapsulated beta-carotene as a function of % RH and its relationship with the physical state of the matrix during storage at 25...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.09.023

    authors: Sutter SC,Buera MP,Elizalde BE

    更新日期:2007-03-06 00:00:00

  • In vitro and in vivo characterization of nanoparticles made of MeO-PEG amine/PLA block copolymer and PLA.

    abstract::The preparative method of a block copolymer of poly(dl-lactic acid) (PLA) and methoxypolyethylene glycol amine (MeO-PEG(N)), named PLA-(MeO-PEG), was refined. The degree of introduction of MeO-PEG(N) into PLA increased up to 55% (mol/mol) using a dichloromethane/methanol mixture (1:1, v/v) as a solvent at the reductiv...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.02.057

    authors: Sasatsu M,Onishi H,Machida Y

    更新日期:2006-07-24 00:00:00

  • Preparation and evaluation of self-nanoemulsified drug delivery systems (SNEDDSs) of matrine based on drug-phospholipid complex technique.

    abstract::To enhance oral bioavailability of matrine, a dedicated and newly emerging drug system called self-nanoemulsifying drug delivery system (SNEDDSs) was developed. Phospholipid complex (MPC) was prepared using solvent-evaporation method to improve the liposolubility of matrine. Solubilization test, infrared spectroscopy ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2009.11.026

    authors: Ruan J,Liu J,Zhu D,Gong T,Yang F,Hao X,Zhang Z

    更新日期:2010-02-15 00:00:00

  • Pluronic gels for nasal delivery of Vitamin B12. Part I: preformulation study.

    abstract::Thermoreversible nasal gels of Vitamin B(12) using pluronic PF 127 were aimed to improve absorption and patient compliance. In the present research work, effects of Vitamin B(12) and gel additives, viz. PF concentration, osmolarity, polyethylene glycol (PEG 15000) on thermodynamic properties of phase transitions at ge...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2003.10.005

    authors: Pisal SS,Paradkar AR,Mahadik KR,Kadam SS

    更新日期:2004-02-11 00:00:00

  • Enhanced oral bioavailability of docetaxel in rats by four consecutive days of pre-treatment with curcumin.

    abstract::As with many other anti-cancer agents, docetaxel is a substrate for ATP-binding cassette transporters such as P-glycoprotein and its metabolism is mainly catalysed by CYP3A. In order to improve the oral bioavailability of docetaxel, a component of turmeric, curcumin, which can down-regulate the intestinal P-glycoprote...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.08.015

    authors: Yan YD,Kim DH,Sung JH,Yong CS,Choi HG

    更新日期:2010-10-31 00:00:00

  • Transdermal permeation of selegiline from hydrogel-membrane drug delivery systems.

    abstract::In the present work, we attempted to design a transdermal system for delivering selegiline using a hydrogel-based drug reservoir and a rate-controlling membrane (Solupor polyethylene membranes). The appearances of these preparations were evaluated by scanning electron microscopy (SEM), and the in vitro skin permeation...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2009.06.025

    authors: Fang JY,Hung CF,Chi CH,Chen CC

    更新日期:2009-10-01 00:00:00

  • Long-circulating non-toxic blood pool imaging agent based on hyperbranched polyglycerols.

    abstract:PURPOSE:Currently, in vivo or in vitro(99m)Tc-radiolabelled red blood cells are the standard blood pool imaging agents. Due to risks associated with handling of blood and the problems with the current (99m)Tc shortage, we were interested in a long-circulating biocompatible synthetic macromolecule that would be simple t...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.10.036

    authors: Saatchi K,Gelder N,Gershkovich P,Sivak O,Wasan KM,Kainthan RK,Brooks DE,Häfeli UO

    更新日期:2012-01-17 00:00:00

  • Achieving delayed release of freeze-dried probiotic strains by extrusion, spheronization and fluid bed coating - evaluated using a three-step in vitro model.

    abstract::Intake of probiotics is associated with many health benefits, which has generated an interest in formulating viable probiotic supplements. The present study had two aims. The first aim was to achieve gastrointestinal protection and delayed release of viable probiotics by pelletizing and coating freeze-dried probiotic ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.120022

    authors: Jacobsen NMY,Caglayan I,Caglayan A,Bar-Shalom D,Müllertz A

    更新日期:2020-12-15 00:00:00

  • Stability study of amorphous valdecoxib.

    abstract::Formulation of poorly water-soluble drugs in the most stable dosage form for oral delivery perhaps presents the greatest challenge to pharmaceutical industry. Physical transformation of drug substance into its more soluble but metastable amorphous form is one of the approaches for improving dissolution rate of such dr...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2004.06.009

    authors: Ambike AA,Mahadik KR,Paradkar A

    更新日期:2004-09-10 00:00:00

  • Preparation and characterization of the ion-fixed mixed micelles with superior stability.

    abstract::The inherent instability of micelles remains a main challenge for antitumor drug delivery, the objective of this study is to prepare and characterize the ion-fixed mixed micelles with significantly improved stability. The mixed micelles and ion-fixed mixed micelles combining the carboxy-containing PLA (PLA-COO(-)) and...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.05.011

    authors: Li Y,Fu Y,Guo H,Zhang L,Huang L,Yang L

    更新日期:2015-07-15 00:00:00

  • 1H NMR quantification of spray dried and spray freeze-dried saccharide carriers in dry powder inhaler formulations.

    abstract::Quantitative analysis using proton NMR (1H qNMR) has been employed in various areas such as pharmaceutical analysis (e.g., dissolution study), vaccines, natural products analysis, metabolites, and macrolide antibiotics in agriculture industry. However, it is not routinely used in the quantification of saccharides in d...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.03.030

    authors: Babenko M,Peron JR,Kaialy W,Calabrese G,Alany RG,ElShaer A

    更新日期:2019-06-10 00:00:00

  • Electrospun nanofiber-based cancer sensors: A review.

    abstract::Cancer is a malignancy engendering enormous global mortality, steering extensive research for early diagnosis and efficacious prognosis leading to emergence of cancer sensing technologies for multitudinous biomarkers. In this context, nanofibers, imparting high surface area, facile production, morphology control, and ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2020.119364

    authors: Mane PP,Ambekar RS,Kandasubramanian B

    更新日期:2020-06-15 00:00:00

  • Rapid microneedle fabrication by heating and photolithography.

    abstract::Many fabrication methods for microneedle (MN) involve harsh conditions and long drying time. This study aims to fabricate a dissolving MN patch in a simple and efficient manner under mild conditions, using a combination of thermal and photo polymerisation. The MN patch was fabricated by pre-polymerisation of vinylpyrr...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.118992

    authors: Kathuria H,Kang K,Cai J,Kang L

    更新日期:2020-02-15 00:00:00

  • Combined effect of liposomalization and addition of glycerol on the transdermal delivery of isosorbide 5-nitrate in rat skin.

    abstract::In this report, we investigated the combined effect of drug liposomalization and addition of glycerol on the transdermal delivery of isosorbide 5-nitrate (ISN) in rat abdominal skin in vitro. Occlusive application of both liposomal and aqueous ISN solution, with and without addition of 5% glycerol, showed that drug li...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.01.052

    authors: Barichello JM,Yamakawa N,Kisyuku M,Handa H,Shibata T,Ishida T,Kiwada H

    更新日期:2008-06-05 00:00:00

  • Improvement of the intestinal membrane permeability of low molecular weight heparin by complexation with stem bromelain.

    abstract::The aim of this study was to investigate the influence of the proteolytic enzyme bromelain on the permeation of heparin across the gastrointestinal epithelial barrier. Stability of the complex and effect of heparin on the enzymatic activity of bromelain was analysed photometrically by measuring bromelain enzymatic act...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.06.042

    authors: Grabovac V,Bernkop-Schnürch A

    更新日期:2006-12-01 00:00:00

  • Optimisation of glutathione conjugation to liposomes quantified with a validated HPLC assay.

    abstract::Glutathione (GSH) grafted onto nanoliposomes (GSH-liposomes) have the potential to enhance drug delivery into the brain. GSH is known to be an unstable tripeptide, however, despite widespread use to promote active transport its stability has been largely ignored to date. Therefore this study focuses on the optimisatio...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.118451

    authors: Reginald-Opara JN,Svirskis D,O'Carroll SJ,Sreebhavan S,Dean JM,Wu Z

    更新日期:2019-08-15 00:00:00

  • Lectin-coated PLGA microparticles: thermoresponsive release and in vitro evidence for enhanced cell interaction.

    abstract::PLGA-microparticles with 4.7 μm in diameter were prepared by the double emulsion technique and loaded with 1.7 μg fluorescein/mg PLGA mimicking a hydrophilic API. In an effort to further elucidate the release and bioadhesive characteristics of lectin-grafted formulations in vitro, the particles were coated with wheat ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.07.025

    authors: Wang XY,Koller R,Wirth M,Gabor F

    更新日期:2012-10-15 00:00:00

  • Ondansetron buccal administration for paediatric use: A comparison between films and wafers.

    abstract::The objective of this study was the development of different solid formulations, such as wafers and films, for buccal administration of ondansetron, a selective and potent antagonist of 5-hydroxytryptamine 3 receptors used in children for the treatment of nausea and vomiting. Wafers and films have been prepared drying...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119228

    authors: Giordani B,Abruzzo A,Prata C,Nicoletta FP,Dalena F,Cerchiara T,Luppi B,Bigucci F

    更新日期:2020-04-30 00:00:00

  • In vitro and in vivo release of dinalbuphine sebacate extended release formulation: Effect of the oil ratio on drug release.

    abstract::Nalbuphine is a semi-synthetic opioid indicated for the relief of moderate to severe pain. Dinalbuphine sebacate (DNS) is a prodrug of nalbuphine for which we have developed long-acting lipophilic formulations in a benzyl benzoate/sesame oil mixture for intramuscular (IM) injection. In this study, we found that the in...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.08.083

    authors: Li CJ,Ku MY,Lu CY,Tien YE,Chern WH,Huang JD

    更新日期:2017-10-05 00:00:00

  • Release kinetics of an amphiphilic photosensitizer by block-polymer nanoparticles.

    abstract::Block-polymer nanoparticles are now well-known candidates for the delivery of various non-soluble drugs to cells. The release of drugs from these nanoparticles is a major concern related to their efficiency as nanovectors and is still not completely deciphered. Various processes have been identified, depending of both...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.09.032

    authors: Kerdous R,Sureau F,Bour A,Bonneau S

    更新日期:2015-11-30 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

  • TR146 cells grown on filters as a model of human buccal epithelium: IV. Permeability of water, mannitol, testosterone and beta-adrenoceptor antagonists. Comparison to human, monkey and porcine buccal mucosa.

    abstract::The objective of the present study was to evaluate the TR146 cell culture model as an in vitro model of human buccal epithelium. For this purpose, the permeability of water, mannitol and testosterone across the TR146 cell culture model was compared to the permeability across human, monkey and porcine buccal mucosa. Fu...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(99)00368-3

    authors: Nielsen HM,Rassing MR

    更新日期:2000-01-25 00:00:00

  • Non-viral gene delivery carrier and its three-dimensional transfection system.

    abstract::An increasing number of non-viral vectors are being developed for the use of gene delivery nowadays, among which cationic polymers and lipoplexes receive most attention. Most of these researches are focused on how to increase the transfection efficiency of non-viral vectors as well as the reduction of toxicity. In thi...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2009.11.006

    authors: He CX,Tabata Y,Gao JQ

    更新日期:2010-02-15 00:00:00

  • Quantifying electrostatic interactions in pharmaceutical solid systems.

    abstract::Triboelectrification of pharmaceutical powders with stainless steel and polymer contact surfaces was investigated. alpha-Lactose monohydrate, from 90 to 125 up to 355-500 microm, was used to quantify electrostatic interactions with negligible powder adhesion to the contact surface. Size fractions down to 53-75 microm ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(01)00784-0

    authors: Rowley G

    更新日期:2001-10-04 00:00:00

  • An approach for chemical stability during melt extrusion of a drug substance with a high melting point.

    abstract::Poorly water-soluble drug substances that exhibit high melting points are difficult to process by melt extrusion due to chemical instability at high temperatures required for processing. The purpose of this study was to extrude meloxicam (melting point 255°C) by optimizing processing parameters and formulation composi...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.03.070

    authors: Haser A,Huang S,Listro T,White D,Zhang F

    更新日期:2017-05-30 00:00:00

  • Properties of solid dispersions of piroxicam in polyvinylpyrrolidone.

    abstract::Solid dispersions of piroxicam were prepared with polyvinylpyrrolidone (PVP) K-17 PF and PVP K-90 by solvent method. The physical state and drug:PVP interaction of solid dispersions and physical mixtures were characterized by X-ray diffraction, Fourier transform infrared (FTIR) spectroscopy and differential scanning c...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(99)00070-8

    authors: Tantishaiyakul V,Kaewnopparat N,Ingkatawornwong S

    更新日期:1999-04-30 00:00:00