A mucoadhesive in situ gel delivery system for paclitaxel.

Abstract:

:MUC1 gene encodes a transmembrane mucin glycoprotein that is overexpressed in human breast cancer and colon cancer. The objective of this study was to develop an in situ gel delivery system containing paclitaxel (PTX) and mucoadhesives for sustained and targeted delivery of anticancer drugs. The delivery system consisted of chitosan and glyceryl monooleate (GMO) in 0.33M citric acid containing PTX. The in vitro release of PTX from the gel was performed in presence and absence of Tween 80 at drug loads of 0.18%, 0.30%, and 0.54% (wt/wt), in Sorensen's phosphate buffer (pH 7.4) at 37 degrees C. Different mucin-producing cell lines (Calu-3>Caco-2) were selected for PTX transport studies. Transport of PTX from solution and gel delivery system was performed in side by side diffusion chambers from apical to basal (A-B) and basal to apical (B-A) directions. In vitro release studies revealed that within 4 hours, only 7.61% +/- 0.19%, 12.0% +/- 0.98%, 31.7% +/- 0.40% of PTX were released from 0.18%, 0.30%, and 0.54% drug-loaded gel formulation, respectively, in absence of Tween 80. However, in presence of surfactant (0.05% wt/vol) in the dissolution medium, percentages of PTX released were 28.1% +/- 4.35%, 44.2% +/- 6.35%, and 97.1% +/- 1.22%, respectively. Paclitaxel has shown a polarized transport in all the cell monolayers with B-A transport 2 to 4 times higher than in the A-B direction. The highest mucin-producing cell line (Calu-3) has shown the lowest percentage of PTX transport from gels as compared with Caco-2 cells. Transport of PTX from mucoadhesive gels was shown to be influenced by the mucin-producing capability of cell.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Jauhari S,Dash AK

doi

10.1208/pt070253

subject

Has Abstract

pub_date

2006-06-02 00:00:00

pages

E53

issue

2

issn

1530-9932

journal_volume

7

pub_type

杂志文章
  • Formulation and in vitro evaluation of xanthan gum or carbopol 934-based mucoadhesive patches, loaded with nicotine.

    abstract::Bilayer nicotine mucoadhesive patches were prepared and evaluated to determine the feasibility of the formulation as a nicotine replacement product to aid in smoking cessation. Nicotine patches were prepared using xanthan gum or carbopol 934 as a mucoadhesive polymers and ethyl cellulose as a backing layer. The patche...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9534-5

    authors: Abu-Huwaij R,Obaidat RM,Sweidan K,Al-Hiari Y

    更新日期:2011-03-01 00:00:00

  • Understanding the tendency of amorphous solid dispersions to undergo amorphous-amorphous phase separation in the presence of absorbed moisture.

    abstract::Formulation of an amorphous solid dispersion (ASD) is one of the methods commonly considered to increase the bioavailability of a poorly water-soluble small-molecule active pharmaceutical ingredient (API). However, many factors have to be considered in designing an API-polymer system, including any potential changes t...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9686-y

    authors: Rumondor AC,Wikström H,Van Eerdenbrugh B,Taylor LS

    更新日期:2011-12-01 00:00:00

  • Formulation and development of extended-release micro particulate drug delivery system of solubilized rifaximin.

    abstract::Rifaximin (RFX), a semi-synthetic antibiotic belonging to BCS class IV category, has been used in the treatment of traveler's diarrhea. An attempt has been made to improve aqueous solubility of RFX in the presence of β-cyclodextrin (β-CD) and hydroxy propyl β-cyclodextrin (HP-β-CD) and control its release in the gut b...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-013-9949-x

    authors: Karanje RV,Bhavsar YV,Jahagirdar KH,Bhise KS

    更新日期:2013-06-01 00:00:00

  • Physicochemical investigations and stability studies of amorphous gliclazide.

    abstract::Gliclazide (GLI), a poorly water-soluble antidiabetic, was transformed into a glassy state by melt quench technique in order to improve its physicochemical properties. Chemical stability of GLI during formation of glass was assessed by monitoring thin-layer chromatography, and an existence of amorphous form was confir...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9760-0

    authors: Jondhale S,Bhise S,Pore Y

    更新日期:2012-06-01 00:00:00

  • Preparation and In Vitro-In Vivo Evaluation of Sustained-Release Matrix Pellets of Capsaicin to Enhance the Oral Bioavailability.

    abstract::Capsaicin has multiple pharmacological activities including antioxidant, anticancer, and anti-inflammatory activities. However, its clinical application is limited due to its poor aqueous solubility, gastric irritation, and low oral bioavailability. This research was aimed at preparing sustained-release matrix pellets...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-015-0352-7

    authors: Zhang Y,Huang Z,Omari-Siaw E,Lu S,Zhu Y,Jiang D,Wang M,Yu J,Xu X,Zhang W

    更新日期:2016-04-01 00:00:00

  • Lectin-Conjugated Clarithromycin and Acetohydroxamic Acid-Loaded PLGA Nanoparticles: a Novel Approach for Effective Treatment of H. pylori.

    abstract::Helicobacter pylori infection remains challenging as it mainly colonized beneath the deep gastric mucosa and adheres to epithelial cells of the stomach. Concanavalin-A (Con-A)-conjugated gastro-retentive poly (lactic-co-glycolic acid) (PLGA) nanoparticles of acetohydroxamic acid (AHA) and clarithromycin (CLR) were pre...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-015-0443-5

    authors: Jain SK,Haider T,Kumar A,Jain A

    更新日期:2016-10-01 00:00:00

  • Polymeric micelles of PEG-PE as carriers of all-trans retinoic acid for stability improvement.

    abstract::The topical application of all-trans retinoic acid (ATRA) is an effective treatment for several skin disorders, including photo-aging. Unfortunately, ATRA is susceptible to light, heat, and oxidizing agents. Thus, this study aimed to investigate the ability of polymeric micelles prepared from polyethylene glycol conju...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9749-0

    authors: Wichit A,Tangsumranjit A,Pitaksuteepong T,Waranuch N

    更新日期:2012-03-01 00:00:00

  • Preformulation studies on solid self-emulsifying systems in powder form containing magnesium aluminometasilicate as porous carrier.

    abstract::The influence of alkaline and the neutral grade of magnesium aluminometasilicate as a porous solid carrier for the liquid self-emulsifying formulation with ibuprofen is investigated. Ibuprofen is dissolved in Labrasol, then this solution is adsorbed on the silicates. The drug to the silicate ratio is 1:2, 1:4, and 1:6...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0247-z

    authors: Krupa A,Szlęk J,Jany BR,Jachowicz R

    更新日期:2015-06-01 00:00:00

  • Liquid proliposomes of nimodipine drug delivery system: preparation, characterization, and pharmacokinetics.

    abstract::To investigate the possibility of liquid proliposomes being carriers for oral delivery, nimodipine liquid proliposomes-based soft capsules (NPSC) were prepared. Nimodipine proliposomes were characterized by transmission electron microscopy (TEM), conversion rate from proliposomes to liposomes, entrapment efficiency, p...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-013-9924-6

    authors: Sun C,Wang J,Liu J,Qiu L,Zhang W,Zhang L

    更新日期:2013-03-01 00:00:00

  • Development and characterization of sorbitan monostearate and sesame oil-based organogels for topical delivery of antimicrobials.

    abstract::The current study explains the development of sorbitan monostearate and sesame oil-based organogels for topical drug delivery. The organogels were prepared by dissolving sorbitan monostearate in sesame oil (70°C). Metronidazole was used as a model antimicrobial. The formulations were characterized using phase contrast...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0223-7

    authors: Singh VK,Pramanik K,Ray SS,Pal K

    更新日期:2015-04-01 00:00:00

  • Characterization and in vitro drug release studies of a natural polysaccharide Terminalia catappa gum (Badam gum).

    abstract::The main objective of the present study is the physicochemical characterization of naturally available Terminalia catappa gum (Badam gum [BG]) as a novel pharmaceutical excipient and its suitability in the development of gastroretentive floating drug delivery systems (GRFDDS) to retard the drug for 12 h when the dosag...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9873-5

    authors: Meka VS,Nali SR,Songa AS,Kolapalli VR

    更新日期:2012-12-01 00:00:00

  • An investigation into the influence of experimental conditions on in vitro drug release from immediate-release tablets of levothyroxine sodium and its relation to oral bioavailability.

    abstract::The aim of this study was to investigate the influence of experimental conditions on levothyroxine sodium release from two immediate-release tablet formulations which narrowly passed the standard requirements for bioequivalence studies. The in vivo study was conducted as randomised, single-dose, two-way cross-over pha...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9660-8

    authors: Kocic I,Homsek I,Dacevic M,Parojcic J,Miljkovic B

    更新日期:2011-09-01 00:00:00

  • Transdermal Microneedles-A Materials Perspective.

    abstract::Transdermal drug delivery is an emerging field in the pharmaceutical remit compared with conventional methods (oral and parenteral). Microneedle (MN)-based devices have gained significant interest as a strategy to overcome the skin's formidable barrier: the stratum corneum. This approach provides a less invasive, more...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-019-1560-3

    authors: Ali R,Mehta P,Arshad MS,Kucuk I,Chang MW,Ahmad Z

    更新日期:2019-12-05 00:00:00

  • Probucol release from novel multicompartmental microcapsules for the oral targeted delivery in type 2 diabetes.

    abstract::In previous studies, we developed and characterised multicompartmental microcapsules as a platform for the targeted oral delivery of lipophilic drugs in type 2 diabetes (T2D). We also designed a new microencapsulated formulation of probucol-sodium alginate (PB-SA), with good structural properties and excipient compati...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0205-9

    authors: Mooranian A,Negrulj R,Al-Sallami HS,Fang Z,Mikov M,Golocorbin-Kon S,Fakhoury M,Watts GF,Matthews V,Arfuso F,Lambros A,Al-Salami H

    更新日期:2015-02-01 00:00:00

  • Acoustic-resonance spectrometry as a process analytical technology for the quantification of active pharmaceutical ingredient in semi-solids.

    abstract::The purpose of this study was to demonstrate acoustic resonance spectrometry (ARS) as an alternative process analytical technology to near infrared (NIR) spectroscopy for the quantification of active pharmaceutical ingredient (API) in semi-solids such as creams, gels, ointments, and lotions. The ARS used for this rese...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt070359

    authors: Medendorp J,Buice RG Jr,Lodder RA

    更新日期:2006-07-14 00:00:00

  • Isolation, Formulation, and Efficacy Enhancement of Morin Emulsified Carriers Against Lung Toxicity in Rats.

    abstract::The present study demonstrates a preparative medium-pressure liquid chromatography (MPLC) method for isolation of Morin besides evaluating its efficacy in comparison with its self-nanoemulsifying drug delivery (SNEDD) and nanoemulsion (NE) systems against in-vivo HgCl2-induced lung toxicity in rats. Morin was isolated...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1072-6

    authors: El-Haddad AE,Sheta NM,Boshra SA

    更新日期:2018-07-01 00:00:00

  • Catechol-Functionalized Alginate Nanoparticles as Mucoadhesive Carriers for Intravesical Chemotherapy.

    abstract::This research aimed to synthesize and evaluate mucoadhesive catechol-functionalized alginate (Cat-Alg) nanoparticles (NPs) for bladder cancer. Cat-Alg was synthesized using coupling chemistry, and the structure was verified using NMR and FT-IR. Cat-Alg NPs were generated by ionic gelation between the synthesized Cat-A...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01752-7

    authors: Sahatsapan N,Ngawhirunpat T,Rojanarata T,Opanasopit P,Patrojanasophon P

    更新日期:2020-07-31 00:00:00

  • Particle size and temperature effect on the physical stability of PLGA nanospheres and microspheres containing Bodipy.

    abstract::The purpose of this study was to investigate the effect of particle size, storage temperature, and duration of storage on the physical stability and morphology of polylactic-co-glycolic acid (PLGA) nanospheres and microspheres. PLGA nanospheres and microspheres containing the fluorescent dye, Bodipy, were prepared in ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt050453

    authors: De S,Robinson DH

    更新日期:2004-09-13 00:00:00

  • The influence of modified pluronic F127 copolymers with higher phase transition temperature on arsenic trioxide-releasing properties and toxicity in a subcutaneous model of rats.

    abstract::Pluronic F127 (PF-127) shows thermoreversible property, which is of the utmost interest in optimizing drug formulation and delivery. However, its hitherto unresolved drawback of a low phase transition temperature (T (tr)) has limited its application in injectable drug delivery systems. We have ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9756-9

    authors: Ma Y,Zhang C,Chen X,Jiang H,Pan S,Easteal AJ,Sun X

    更新日期:2012-06-01 00:00:00

  • Preparation and Characterization of PLGA-PEG-PLGA Nanoparticles Containing Salidroside and Tamoxifen for Breast Cancer Therapy.

    abstract::Nanoparticles (NPs) containing the hydrophilic drug salidroside (Sal) and the hydrophobic drug tamoxifen (Tam) were prepared using a triblock copolymer poly(lactic-co-glycolic acid) (PLGA)-poly(ethylene glycol) (PEG)-PLGA to achieve synergism in the treatment of breast cancer. The double emulsion (w/o/w) method was us...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1523-8

    authors: Yu X,Sun L,Tan L,Wang M,Ren X,Pi J,Jiang M,Li N

    更新日期:2020-01-29 00:00:00

  • Pluronic-Based Mixed Polymeric Micelles Enhance the Therapeutic Potential of Curcumin.

    abstract::Curcumin is a naturally occurring constituent of turmeric that is a good substitute for synthetic medicines for the treatment of different diseases, due to its comparatively safer profile. However, there are certain shortcomings that limit its use as an ideal therapeutic agent. In order to overcome these drawbacks, we...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1098-9

    authors: Akbar MU,Zia KM,Nazir A,Iqbal J,Ejaz SA,Akash MSH

    更新日期:2018-08-01 00:00:00

  • Co-solvent evaporation method for enhancement of solubility and dissolution rate of poorly aqueous soluble drug simvastatin: in vitro-in vivo evaluation.

    abstract::A number of synthesized chemical molecules suffer from low aqueous solubility problems. Enhancement of aqueous solubility, dissolution rate, and bioavailability of drug is a very challenging task in drug development. In the present study, solubility and dissolution of poorly aqueous soluble drug simvastatin (SIM) was ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9176-z

    authors: Pandya P,Gattani S,Jain P,Khirwal L,Surana S

    更新日期:2008-01-01 00:00:00

  • Potential Use of Cyclodextrin Complexes for Enhanced Stability, Anti-inflammatory Efficacy, and Ocular Bioavailability of Loteprednol Etabonate.

    abstract::Loteprednol etabonate (LE) is a soft corticosteroid that maintains therapeutic activity with much reduced adverse effects. Yet, its ocular bioavailability is hindered by its poor aqueous solubility. Early attempts of LE complexation with cyclodextrins (CDs) did not involve the study of the effects of various complexat...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0589-9

    authors: Soliman OAE,Mohamed EAM,El-Dahan MS,Khatera NAA

    更新日期:2017-05-01 00:00:00

  • Kinetic modelling for the assay of nortriptyline hydrochloride using potassium permanganate as oxidant.

    abstract::Kinetic methods for accurate determination of nortriptyline hydrochloride have been described. The methods are based on the oxidation of nortriptyline hydrochloride with KMnO4 in acidic and basic media. In acidic medium, the decrease in absorbance at 525.5 nm and in basic medium, the increase in absorbance at 608.5 nm...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0230-8

    authors: Rahman N,Khan S

    更新日期:2015-06-01 00:00:00

  • Development of spray dried liposomal dry powder inhaler of Dapsone.

    abstract::This investigation was undertaken to evaluate practical feasibility of site specific pulmonary delivery of liposomal encapsulated Dapsone (DS) dry powder inhaler for prolonged drug retention in lungs as an effective alternative in prevention of Pneumocystis carinii pneumonia (PCP) associated with immunocompromised pat...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-007-9024-6

    authors: Chougule M,Padhi B,Misra A

    更新日期:2008-01-01 00:00:00

  • Development and evaluation of cetirizine HCl taste-masked oral disintegrating tablets.

    abstract::The purpose of the current study was to mask the taste of cetirizine HCl and to incorporate the granules produced in oral disintegrating tablets (ODT). The bitter, active substance was coated by fluidized bed coating using Eudragit® RL30-D at levels between 15% and 40% w/w. The ODTs were developed by varying the ratio...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9569-7

    authors: Douroumis DD,Gryczke A,Schminke S

    更新日期:2011-03-01 00:00:00

  • Rheological characterization of neutral and anionic polysaccharides with reduced mucociliary transport rates.

    abstract::The purpose of this research was to compare the viscoelastic properties of several neutral and anionic polysaccharide polymers with their mucociliary transport rates (MTR) across explants of ciliated bovine tracheal tissue to identify rheologic parameters capable of predicting the extent of reduction in mucociliary tr...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt0802032

    authors: Shah AJ,Donovan MD

    更新日期:2007-04-20 00:00:00

  • Optimization of an aqueous tablet-coating process containing carboxymethylated Cassia fistula gum.

    abstract::The present investigation was aimed at developing and optimizing a simple aqueous tablet-coating formulation and its process. 5-Fluorouracil (5-FU) was used to ascertain the relative lipophilic/hydrophilic behavior of the coating system. Optimization was performed by evaluating the adhesive force strength and cohesive...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9763-x

    authors: Rai PR,Tiwary AK,Rana V

    更新日期:2012-06-01 00:00:00

  • 3D-Printed Isoniazid Tablets for the Treatment and Prevention of Tuberculosis-Personalized Dosing and Drug Release.

    abstract::The aim of the present work was to produce 3D-printed oral dosage forms with a sufficient drug dose displaying various release profiles. Hot-melt extrusion was utilized to produce drug-loaded feedstock material that was subsequently 3D-printed into 6, 8, and 10 × 2.5 mm tablets with 15% and 90% infill levels. The prep...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1233-7

    authors: Öblom H,Zhang J,Pimparade M,Speer I,Preis M,Repka M,Sandler N

    更新日期:2019-01-07 00:00:00

  • Formulation Optimization and Ex Vivo and In Vivo Evaluation of Celecoxib Microemulsion-Based Gel for Transdermal Delivery.

    abstract::Celecoxib (CXB) is a poorly aqueous solubility sulfonamide non-steroidal anti-inflammatory drug (NSAID). Hence, the formulation of CXB was selected for solubilization and bioavailability. To find out suitable formulation for microemulsion, the solubility of CXB in triacetin (oil phase), Tween 80 (surfactant), and Tran...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0667-z

    authors: Cao M,Ren L,Chen G

    更新日期:2017-08-01 00:00:00