Evidence map›Paper›PMID 26286185›Full record

ArticlePharmaceutical research2016

Novel Gefitinib Formulation with Improved Oral Bioavailability in Treatment of A431 Skin Carcinoma.

Chandraiah Godugu, Ravi Doddapaneni, Apurva R Patel, Rakesh Singh, Roger Mercer, Mandip Singh

Abstract read
In one paragraph

Article in Pharmaceutical research, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
1.1field-weighted citation impact, top 24% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

14 citing papers in PubMed, 46 citations in OpenAlex.

  1. Article
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  8. Modified gefitinib conjugated FeFrontiers in bioengineering and biotechnology · 2023
    Article
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  14. Novel diindolylmethane derivatives based NLC formulations to improve the oral bioavailability and anticancer effects in triple negative breast cancer.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2016
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors at 3 institutions in 2 countries.

Chandraiah GoduguCollege of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, Florida, USA.
Ravi DoddapaneniCollege of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, Florida, USA.
Apurva R PatelCollege of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, Florida, USA.
Rakesh SinghTranslational Science Laboratory, Florida State University, College of Medicine, Tallahassee, Florida, 32306, USA.
Roger MercerTranslational Science Laboratory, Florida State University, College of Medicine, Tallahassee, Florida, 32306, USA.
Mandip SinghCollege of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, Florida, USA. mandip.sachdeva@famu.edu.
Florida Agricultural and Mechanical University · USFlorida State University · USNational Institute of Pharmaceutical Education and Research · IN

Funding

THE PREVENTION OF B(A)P INDUCED CELL TRANSFORMATION BY ORGANOSULFUR COMPOUNDSG12RR003020 · NCRR · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI SOLIMAN, KARAM F.A. · 1985 to 2011
$29.7M
Recruitment and HiringG12MD007582 · NIMHD · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI SOLIMAN, KARAM F.A. · 2012 to 2017
$16.0M
Targeted Nanocarrier Combination Based Therapy for Lung CancerP20MD006738 · NIMHD · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI RAHMAN, SALEH MD. MAHMUDUR · 2012 to 2016
$5.6M
Targeted Nanocarriers for Treatment of Lung CancerSC1CA161676 · NCI · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI SACHDEVA, MANDIP SINGH · 2011 to 2014
$1.1M
NCI NIH HHS 5SC1CA161676-03NCI NIH HHS SC1 CA161676NCRR NIH HHS G12 RR003020NIMHD NIH HHS 1P20MD006738-03NIMHD NIH HHS G12 MD007582NIMHD NIH HHS P20 MD006738
6 · The paper itself

Abstract

purposeOral administration of anticancer agents presents a series of advantages for patients. However, most of the anticancer drugs have poor water solubility leading to low bioavailability.

methodsControlled released spray dried matrix system of Gefitinib with hydroxypropyl β-cyclodextrin, chitosan, hydroxy propyl methyl cellulose, vitamin E TPGS, succinic acid were used for the design of formulations to improve the oral absorption of Gefitinib. Spray drying with a customized spray gun which allows simultaneous/pulsatile flow of two different liquid systems through single nozzle was used to prepare Gefitinib spray dried formulations (Gef-SD). Formulation was characterized by in vitro drug release and Caco-2 permeability studies. Pharmacokinetic studies were performed in Sprague Dawley rats. Efficacy of Gef-SD was carried out in A431 xenografts models in nude mice.

resultsIn Gef-SD group 9.14-fold increase in the AUC was observed compared to free Gef. Improved pharmacokinetic profile of Gef-SD translated into increase (1.75 fold compared to Gef free drug) in anticancer effects. Animal survival was significantly increased in Gef formulation treated groups, with superior reduction in the tumor size (1.48-fold) and volumes (1.75-fold) and also increase in the anticancer effects (TUNEL positive apoptotic cells) was observed in Gef-SD treated groups. Further, western blot, immunohistochemical and proteomics analysis demonstrated the increased pharmacodynamic effects of Gef-SD formulations in A431 xenograft tumor models.

conclusionOur studies suggested that Gefitinib can be successfully incorporated into control release microparticles based oral formulation with enhanced pharmacokinetic and pharmacodynamic activity. This study demonstrates the novel application of Gef in A431 tumor models.

Indexed as

AnimalsAntineoplastic AgentsArea Under CurveBiological AvailabilityCaco-2 CellsCarcinoma, Squamous CellCell Line, TumorChemistry, PharmaceuticalExcipientsGefitinibHumansMice, NudeProteomicsQuinazolinesRatsRats, Sprague-DawleyAntineoplastic AgentsExcipientsGefitinibQuinazolinesA431control release formulationsepidermal growth factor receptorgefitinibspray drying

Identifiers

PMID26286185
PMCPMC4774891
OpenAlexW1515631506

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.