Online citations, reference lists, and bibliographies.
← Back to Search

Development And Characterization Of Chitosan Microparticles-in-Films For Buccal Delivery Of Bioactive Peptides

P. Batista, P. Castro, A. R. Madureira, B. Sarmento, M. Pintado
Published 2019 · Medicine

Cite This
Download PDF
Analyze on Scholarcy
Share
Nowadays, bioactive peptides are used for therapeutic applications and the selection of a carrier to deliver them is very important to increase the efficiency, absorption, release, bioavailability and consumer acceptance. The aim of this study was to develop and characterize chitosan-based films loaded with chitosan microparticles containing a bioactive peptide (sequence: KGYGGVSLPEW) with antihypertensive properties. Films were prepared by the solvent casting method, while the microparticles were prepared by ionic gelation. The final optimized chitosan microparticles exhibited a mean diameter of 2.5 µm, a polydispersity index of 0.46, a zeta potential of +61 mV and a peptide association efficiency of 76%. Chitosan films were optimized achieving the final formulation of 0.79% (w/v) of chitosan, 6.74% (w/v) of sorbitol and 0.82% (w/v) of citric acid. These thin (±0.100 mm) and transparent films demonstrated good performance in terms of mechanical and biological properties. The oral films developed were flexible, elastic, easy to handle and exhibited rapid disintegration (30 s) and an erosion behavior of 20% when they came into contact with saliva solution. The cell viability (75–99%) was proved by methylthiazolydiphenyl-tetrazolium bromide (MTT) assay with TR146 cells. The chitosan mucoadhesive films loaded with peptide–chitosan microparticles resulted in an innovative approach to perform administration across the buccal mucosa, because these films present a larger surface area, leading to the rapid disintegration and release of the antihypertensive peptide under controlled conditions in the buccal cavity, thus promoting bioavailability.
This paper references
10.1016/j.colsurfb.2013.07.019
An integrated buccal delivery system combining chitosan films impregnated with peptide loaded PEG-b-PLA nanoparticles.
Concetta Giovino (2013)
10.2174/156720109789941713
A review on mouth dissolving films.
Meenu Dahiya (2009)
Bhatnagar, I. Chitosan as biomaterial in drug delivery and tissue engineering
S M Ahsan (2017)
10.1016/j.carbpol.2017.06.090
Microparticles prepared with 50-190kDa chitosan as promising non-toxic carriers for pulmonary delivery of isoniazid.
Paula M Oliveira (2017)
10.1016/j.peptides.2011.02.005
Novel whey-derived peptides with inhibitory effect against angiotensin-converting enzyme: In vitro effect and stability to gastrointestinal enzymes
T. Tavares (2011)
10.1016/J.FOODHYD.2016.06.034
Preparation, characterization, and properties of chitosan films with cinnamaldehyde nanoemulsions
Huanle Chen (2016)
10.3109/1061186X.2011.628397
Nanocarrier possibilities for functional targeting of bioactive peptides and proteins: state-of-the-art
Carla Guimarães Moutinho (2012)
10.1016/J.FOODRES.2015.01.016
Whey as a source of peptides with remarkable biological activities
A. Brandelli (2015)
Preparation, characterization, and potential application of chitosan, chitosan derivatives, and chitosan metal nanoparticles in pharmaceutical drug delivery. Drug Des
T A Ahmed (2016)
10.1080/03639040902744704
Development and mechanical characterization of solvent-cast polymeric films as potential drug delivery systems to mucosal surfaces
J. Boateng (2009)
GRAS Notice Inventory
P. Calvo
Buccal Film: An Advance Technology for Oral Drug Delivery
S. Verma (2014)
10.1016/j.peptides.2018.01.002
Recent insights in the use of nanocarriers for the oral delivery of bioactive proteins and peptides
P. Batista (2018)
10.1016/j.carbpol.2015.04.020
Fabrication of chitosan microspheres using vanillin/TPP dual crosslinkers for protein antigens encapsulation.
S. Walke (2015)
10.1016/j.ijpharm.2018.05.051
Combination of PLGA nanoparticles with mucoadhesive guar‐gum films for buccal delivery of antihypertensive peptide
P. Castro (2018)
10.1615/CRITREVTHERDRUGCARRIERSYST.V20.I23.30
Emerging trends in oral delivery of peptide and protein drugs.
R. Mahato (2003)
10.2147/IJN.S17296
Recent advances of chitosan nanoparticles as drug carriers
J. Wang (2011)
10.1016/j.ijpharm.2012.02.035
Development and characterisation of chitosan films impregnated with insulin loaded PEG-b-PLA nanoparticles (NPs): a potential approach for buccal delivery of macromolecules.
Concetta Giovino (2012)
10.1016/S0378-5173(99)00368-3
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.
H. M. Nielsen (2000)
10.1016/j.ejpb.2016.04.001
Development of fast dissolving oral films containing lercanidipine HCl nanoparticles in semicrystalline polymeric matrix for enhanced dissolution and ex vivo permeation.
Ankita D. Chonkar (2016)
10.1002/APP.31136
In vitro degradation of starch/PVA films and biocompatibility evaluation
Rui Shi (2010)
10.1023/A:1014220832384
The Potential of Chitosan in Enhancing Peptide and Protein Absorption Across the TR146 Cell Culture Model—An in Vitro Model of the Buccal Epithelium
A. Portero (2004)
Novel whey - derived
T. Tavares
10.1002/(SICI)1097-4628(19970103)63:1<125::AID-APP13>3.0.CO;2-4
Novel hydrophilic chitosan‐polyethylene oxide nanoparticles as protein carriers
P. Calvo (1997)
10.1016/J.FOODHYD.2015.05.023
Biological effects of chitosan and its derivatives
Dai-Hung Ngo (2015)
10.2174/157016311796799035
Chitosan formulations as carriers for therapeutic proteins.
Fernanda Andrade (2011)
10.1016/j.ijpharm.2014.07.039
Preparation of ibuprofen-loaded chitosan films for oral mucosal drug delivery using supercritical solution impregnation.
C. Tang (2014)
10.4103/0250-474X.42967
Protein and Peptide Drug Delivery: Oral Approaches
J. Shaji (2008)
and Drug Administration
US Foo (2008)
10.1016/j.carbpol.2016.03.077
Insightful understanding of the role of clay topology on the stability of biomimetic hybrid chitosan-clay thin films and CO2-dried porous aerogel microspheres.
S. Frindy (2016)
10.1021/JF034612P
Incorporation of a high concentration of mineral or vitamin into chitosan-based films.
Su-il Park (2004)
10.1016/S0142-9612(00)00115-0
The manufacturing techniques of various drug loaded biodegradable poly(lactide-co-glycolide) (PLGA) devices.
R. Jain (2000)
10.1080/00914037.2015.1030661
Development of Oral Strips Containing Chitosan as Active Ingredient: A Product for Buccal Health
A. Cardelle-Cobas (2015)
10.1016/J.JFOODENG.2014.12.020
Protein adsorption onto alginate-pectin microparticles and films produced by ionic gelation
Karla Aguilar (2015)
10.1016/j.msec.2013.10.038
Improvement in antihypertensive and antianginal effects of felodipine by enhanced absorption from PLGA nanoparticles optimized by factorial design.
U. Shah (2014)
10.1016/j.ddtec.2005.05.018
Buccal drug delivery: A challenge already won?
S. Rossi (2005)
10.1016/J.BEJ.2014.11.008
Scalable production of highly concentrated chitosan/TPP nanoparticles in different pHs and evaluation of the in vitro transfection efficiency
C. C. Sipoli (2015)
10.1016/j.msec.2017.02.173
Optimization of two biopolymer-based oral films for the delivery of bioactive molecules.
Pedro M. Castro (2017)
10.1016/j.biomaterials.2014.07.026
The impact of nanoparticles on the mucosal translocation and transport of GLP-1 across the intestinal epithelium.
F. Araújo (2014)
American Guidance for Industry: Orally Disintegrating Tablets; US Food and Drug Administration
(2008)
10.1016/j.ijbiomac.2017.03.163
Properties of gelatin-based films incorporated with chitosan-coated microparticles charged with rutin.
Ilyes Dammak (2017)
10.1016/J.JBIOTEC.2010.10.057
Development and evaluation of a novel biodegradable film made from chitosan and cinnamon essential oil with low affinity toward water
M. Rezaei (2010)
10.3390/ijms17121977
Enhanced and Extended Anti-Hypertensive Effect of VP5 Nanoparticles
Ting Yu (2016)
10.1016/j.jconrel.2015.05.258
Oral films as breakthrough tools for oral delivery of proteins/peptides.
P. Castro (2015)
10.1016/j.jsps.2015.02.024
Orally disintegrating films: A modern expansion in drug delivery system
M. Irfan (2016)
10.4155/tde.14.5
Recent developments in protein and peptide parenteral delivery approaches.
Ashaben Patel (2014)
10.1016/J.DRUDIS.2006.08.005
Is the oral route possible for peptide and protein drug delivery?
M. Morishita (2006)
10.1016/j.jconrel.2015.10.012
Nanotechnology for protein delivery: Overview and perspectives.
Mikyung Yu (2016)
10.3390/md14050090
Effect of Experimental Parameters on Alginate/Chitosan Microparticles for BCG Encapsulation
Liliana Aranha Caetano (2016)
10.2147/DDDT.S99651
Preparation, characterization, and potential application of chitosan, chitosan derivatives, and chitosan metal nanoparticles in pharmaceutical drug delivery
T. Ahmed (2016)
10.1016/j.ijbiomac.2017.08.140
Chitosan as biomaterial in drug delivery and tissue engineering.
Saad M Ahsan (2018)
10.1016/j.colsurfb.2014.04.024
Development and characterization of GRGDSPC-modified poly(lactide-co-glycolide acid) porous microspheres incorporated with protein-loaded chitosan microspheres for bone tissue engineering.
Chun Tao (2014)
10.1016/j.carbpol.2015.10.012
Fabrication, characterization and cytotoxicity studies of ionically cross-linked docetaxel loaded chitosan nanoparticles.
Ankit Jain (2016)



This paper is referenced by
10.3390/polym11071226
Adsorption of Vi Capsular Antigen of Salmonella Typhi in Chitosan–Poly (Methacrylic Acid) Nanoparticles
Raimundo Lopes da Silva (2019)
10.1007/s13346-020-00708-5
A chitosan film containing quercetin-loaded transfersomes for treatment of secondary osteoporosis
Ashlesha P Pandit (2020)
10.3390/ph13090203
Development and Characterization of Inkjet Printed Edible Films for Buccal Delivery of B-Complex Vitamins
Georgios K Eleftheriadis (2020)
10.21608/EJCHEM.2019.11668.1743
Characterization of Chitosan and Polyethylene glycol Blend Film
A. Sarhan (2019)
10.1016/j.ijpharm.2019.118578
In vitro antibacterial activity of ciprofloxacin loaded chitosan microparticles and their effects on human lung epithelial cells.
Vildan Kucukoglu (2019)
10.1007/s40204-020-00139-y
Recent advances in the formulation of PLGA microparticles for controlled drug delivery
Elena Lagreca (2020)
10.3390/biom9090470
Progress in the Development of Chitosan-Based Biomaterials for Tissue Engineering and Regenerative Medicine
Bolat Sultankulov (2019)
10.1016/j.jare.2020.04.019
Enhanced pharmacokinetic performance of dapoxetine hydrochloride via the formulation of instantly-dissolving buccal films with acidic pH modifier and hydrophilic cyclodextrin: Factorial analysis, in vitro and in vivo assessment
Hibah M Aldawsari (2020)
10.1016/j.carbpol.2020.116724
Supramolecular aggregates of cyclodextrins with co-solvent modulate drug dispersion and release behavior of poorly soluble corticosteroid from chitosan membranes.
E. G. do Nascimento (2020)
10.1016/j.porgcoat.2020.105707
Efficient reinforcement of chitosan-based coatings for Ricotta cheese with non-toxic, active, and smart nanoparticles
Andreii S. Kritchenkov (2020)
10.1002/cbic.201900242
Biocompatible Inhibitor Based on Chitosan and Amphiphilic Peptide against Mutant Huntingtin Toxicity
D. Wahyuningtyas (2019)
Semantic Scholar Logo Some data provided by SemanticScholar