← 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
Download PDFAnalyze on Scholarcy
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
An integrated buccal delivery system combining chitosan films impregnated with peptide loaded PEG-b-PLA nanoparticles.
Concetta Giovino (2013)
A review on mouth dissolving films.
Meenu Dahiya (2009)
Bhatnagar, I. Chitosan as biomaterial in drug delivery and tissue engineering
S M Ahsan (2017)
Microparticles prepared with 50-190kDa chitosan as promising non-toxic carriers for pulmonary delivery of isoniazid.
Paula M Oliveira (2017)
Novel whey-derived peptides with inhibitory effect against angiotensin-converting enzyme: In vitro effect and stability to gastrointestinal enzymes
T. Tavares (2011)
Preparation, characterization, and properties of chitosan films with cinnamaldehyde nanoemulsions
Huanle Chen (2016)
Nanocarrier possibilities for functional targeting of bioactive peptides and proteins: state-of-the-art
Carla Guimarães Moutinho (2012)
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)
Development and mechanical characterization of solvent-cast polymeric films as potential drug delivery systems to mucosal surfaces
J. Boateng (2009)
GRAS Notice Inventory
Buccal Film: An Advance Technology for Oral Drug Delivery
S. Verma (2014)
Recent insights in the use of nanocarriers for the oral delivery of bioactive proteins and peptides
P. Batista (2018)
Fabrication of chitosan microspheres using vanillin/TPP dual crosslinkers for protein antigens encapsulation.
S. Walke (2015)
Combination of PLGA nanoparticles with mucoadhesive guar‐gum films for buccal delivery of antihypertensive peptide
P. Castro (2018)
Emerging trends in oral delivery of peptide and protein drugs.
R. Mahato (2003)
Recent advances of chitosan nanoparticles as drug carriers
J. Wang (2011)
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)
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)
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)
In vitro degradation of starch/PVA films and biocompatibility evaluation
Rui Shi (2010)
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
Novel hydrophilic chitosan‐polyethylene oxide nanoparticles as protein carriers
P. Calvo (1997)
Biological effects of chitosan and its derivatives
Dai-Hung Ngo (2015)
Chitosan formulations as carriers for therapeutic proteins.
Fernanda Andrade (2011)
Preparation of ibuprofen-loaded chitosan films for oral mucosal drug delivery using supercritical solution impregnation.
C. Tang (2014)
Protein and Peptide Drug Delivery: Oral Approaches
J. Shaji (2008)
and Drug Administration
US Foo (2008)
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)
Incorporation of a high concentration of mineral or vitamin into chitosan-based films.
Su-il Park (2004)
The manufacturing techniques of various drug loaded biodegradable poly(lactide-co-glycolide) (PLGA) devices.
R. Jain (2000)
Development of Oral Strips Containing Chitosan as Active Ingredient: A Product for Buccal Health
A. Cardelle-Cobas (2015)
Protein adsorption onto alginate-pectin microparticles and films produced by ionic gelation
Karla Aguilar (2015)
Improvement in antihypertensive and antianginal effects of felodipine by enhanced absorption from PLGA nanoparticles optimized by factorial design.
U. Shah (2014)
Buccal drug delivery: A challenge already won?
S. Rossi (2005)
Scalable production of highly concentrated chitosan/TPP nanoparticles in different pHs and evaluation of the in vitro transfection efficiency
C. C. Sipoli (2015)
Optimization of two biopolymer-based oral films for the delivery of bioactive molecules.
Pedro M. Castro (2017)
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
Properties of gelatin-based films incorporated with chitosan-coated microparticles charged with rutin.
Ilyes Dammak (2017)
Development and evaluation of a novel biodegradable film made from chitosan and cinnamon essential oil with low affinity toward water
M. Rezaei (2010)
Enhanced and Extended Anti-Hypertensive Effect of VP5 Nanoparticles
Ting Yu (2016)
Oral films as breakthrough tools for oral delivery of proteins/peptides.
P. Castro (2015)
Orally disintegrating films: A modern expansion in drug delivery system
M. Irfan (2016)
Recent developments in protein and peptide parenteral delivery approaches.
Ashaben Patel (2014)
Is the oral route possible for peptide and protein drug delivery?
M. Morishita (2006)
Nanotechnology for protein delivery: Overview and perspectives.
Mikyung Yu (2016)
Effect of Experimental Parameters on Alginate/Chitosan Microparticles for BCG Encapsulation
Liliana Aranha Caetano (2016)
Preparation, characterization, and potential application of chitosan, chitosan derivatives, and chitosan metal nanoparticles in pharmaceutical drug delivery
T. Ahmed (2016)
Chitosan as biomaterial in drug delivery and tissue engineering.
Saad M Ahsan (2018)
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)
Fabrication, characterization and cytotoxicity studies of ionically cross-linked docetaxel loaded chitosan nanoparticles.
Ankit Jain (2016)
This paper is referenced by
Adsorption of Vi Capsular Antigen of Salmonella Typhi in Chitosan–Poly (Methacrylic Acid) Nanoparticles
Raimundo Lopes da Silva (2019)
A chitosan film containing quercetin-loaded transfersomes for treatment of secondary osteoporosis
Ashlesha P Pandit (2020)
Development and Characterization of Inkjet Printed Edible Films for Buccal Delivery of B-Complex Vitamins
Georgios K Eleftheriadis (2020)
Characterization of Chitosan and Polyethylene glycol Blend Film
A. Sarhan (2019)
In vitro antibacterial activity of ciprofloxacin loaded chitosan microparticles and their effects on human lung epithelial cells.
Vildan Kucukoglu (2019)
Recent advances in the formulation of PLGA microparticles for controlled drug delivery
Elena Lagreca (2020)
Progress in the Development of Chitosan-Based Biomaterials for Tissue Engineering and Regenerative Medicine
Bolat Sultankulov (2019)
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)
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)
Efficient reinforcement of chitosan-based coatings for Ricotta cheese with non-toxic, active, and smart nanoparticles
Andreii S. Kritchenkov (2020)
Biocompatible Inhibitor Based on Chitosan and Amphiphilic Peptide against Mutant Huntingtin Toxicity
D. Wahyuningtyas (2019)