Locust bean gum hydrogels are bioadhesive and improve indole-3-carbinol cutaneous permeation

influence of the polysaccharide concentration

Authors

  • Carina Dinah Merg Laboratório de Tecnologia Farmacêutica, Departamento de Farmácia Industrial, Universidade Federal de Santa Maria Santa Maria, RS, Brazil
  • Jéssica Brandão Reolon Laboratório de Tecnologia Farmacêutica, Departamento de Farmácia Industrial, Universidade Federal de Santa Maria Santa Maria, RS, Brazil
  • Giancarlo Cervo Rechia Escola de Medicina, Universidade Franciscana, Santa Maria, RS, Brazil
  • Letícia Cruz Laboratório de Tecnologia Farmacêutica, Departamento de Farmácia Industrial, Universidade Federal de Santa Maria Santa Maria, RS, Brazil https://orcid.org/0000-0001-6230-4577

DOI:

https://doi.org/10.1590/s2175-97902023e21770%20

Keywords:

Locust bean gum, Topical application, Hydrogels, Indole-3-carbinol, Skin permeation

Abstract

The locust bean gum (LBG) is a polysaccharide with thickening, stabilizing and gelling properties and it has been used in the preparation of pharmaceutical formulations. Hydrogels (HGs) are obtained from natural or synthetic materials that present interesting properties for skin application. This study aimed to develop HGs from LBG using indole-3-carbinol (I3C) as an asset model for cutaneous application. HGs were prepared by dispersing LBG (2%, 3% and 4% w/v) directly in cold water. The formulations showed content close to 0.5 mg/g (HPLC) and pH ranging from 7.25 to 7.41 (potentiometry). The spreadability factor (parallel plate method) was inversely proportional to LBG concentration. The rheological evaluation (rotational viscometer) demonstrated a non-Newtonian pseudoplastic flow behavior (Ostwald De Weale model), which is interesting for cutaneous application. The HET-CAM evaluation showed the non-irritating characteristic of the formulations. The bioadhesive potential demonstrated bioadhesion in a concentration-dependent manner. Permeation in human skin using Franz cells showed that the highest LBG concentration improved the skin distribution profile with greater I3C amounts in the viable skin layers. The present study demonstrated the feasibility of preparing HGs with LBG and the formulation with the highest polymer concentration was the most promising to transport active ingredients through the skin.

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References

Ahmad A, Sakr WA, Wahidur Rahman KM. Mechanisms and therapeutic implications of cell death induction by indole compounds. Cancers (Basel) 2011;3(3):2955-2974. doi: 10.3390/cancers3032955

» https://doi.org/10.3390/cancers3032955

Ahmad S, Ahmad M, Manzoor K, Purwar R, Ikram S. A review on latest innovations in natural gums based hydrogels: Preparations & applications. Int J Biol Macromol 2019;136:870-890. doi: 10.1016/j.ijbiomac.2019.06.113

» https://doi.org/10.1016/j.ijbiomac.2019.06.113

Akkaya NE, Ergun C, Saygun A, Yesilcubuk N, Akel-Sadoglu N, Kavakli H, et al. New biocompatible antibacterial wound dressing candidates; agar-locust bean gum and agar-salep films. Int J Biol Macromol 2020;155:430-438. doi: 10.1016/j.ijbiomac.2020.03.214

» https://doi.org/10.1016/j.ijbiomac.2020.03.214

Banerjee S, Kong D, Wang Z, Bao B, Hillman GG, Sarkar FH. Attenuation of multi-targeted proliferation-linked signaling by 3,3’-diindolylmethane (DIM): From bench to clinic. Mutat Res - Rev Mutat Res 2011;728(1-2):47-66. doi: 10.1016/j.mrrev.2011.06.001

» https://doi.org/10.1016/j.mrrev.2011.06.001

Barakat NS. Evaluation of glycofurol-based gel as a new vehicle for topical application of Naproxen. AAPS PharmSciTech 2010;11(3):1138-1146. doi: 10.1208/s12249-010-9485-x

» https://doi.org/10.1208/s12249-010-9485-x

Calixto G, Yoshii AC, Silva HR, Cury BSF, Chorilli M. Polyacrylic acid polymers hydrogels intended to topical drug delivery: Preparation and characterization. Pharm Dev Technol 2015;20(4):490-496. doi: 10.3109/10837450.2014.882941

» https://doi.org/10.3109/10837450.2014.882941

Cazorla-Luna R, Martín-Illana A, Notario-Pérez F, Bedoya LM, Bermejo P, Ruiz-Caro R, et al. Dapivirine bioadhesive vaginal tablets based on natural polymers for the prevention of sexual transmission of HIV. Polymers (Basel) 2019;11(3):1-17. doi: 10.3390/polym11030483

» https://doi.org/10.3390/polym11030483

Chin JS, Madden L, Chew SY, Becker DL. Drug therapies and delivery mechanisms to treat perturbed skin wound healing. Adv Drug Deliv Rev 2019;149-150:2-18. doi: 10.1016/j.addr.2019.03.006

» https://doi.org/10.1016/j.addr.2019.03.006

Coviello T, Trotta AM, Marianecci C, Carafa M, Di Marzio L, Rinaldi F, et al. Gel-embedded niosomes: Preparation, characterization and release studies of a new system for topical drug delivery. Colloids Surfaces B Biointerfaces 2015;125:291-299. doi: 10.1016/j.colsurf b.2014.10.060

» https://doi.org/10.1016/j.colsurf b.2014.10.060

Dalla Lana DF, Lavorato SN, Giuliani LM, Cruz L, Lopes W, Vainstein MH, et al. Discovery of a novel and selective fungicide that targets fungal cell wall to treat dermatomycoses: 1,3-bis(3,4-dichlorophenoxy)propan-2-aminium chloride. Mycoses 2020;63(2):197-211. doi: 10.1111/myc.13027

» https://doi.org/10.1111/myc.13027

Debebe D, Gabriel T, Brhane Y, Temesgen A, Nigatu M, Marew T. Comparative in vitro evaluation of brands of clotrimazole cream formulations marketed in Ethiopia. J Drug Deliv Ther 2018;8(1):17-22. doi: 10.22270/jddt.v8i1.1546

» https://doi.org/10.22270/jddt.v8i1.1546

Deshmukh VN, Jadhav JK, Sakarkar DM. Formulation and in vitro evaluation of theophylline anhydrous bioadhesive tablets. Asian J Pharm 2009;3(1):54-58. doi: 10.4103/0973-8398.49176

» https://doi.org/10.4103/0973-8398.49176

Ferreira LM, Sari MHM, Azambuja JH, Silveira EF, Cervi VF, Marchiori MCL, et al. Xanthan gum-based hydrogel containing nanocapsules for cutaneous diphenyl diselenide delivery in melanoma therapy. Invest New Drugs 2020;38(3):662-674. doi: 10.1007/s10637-019-00823-2

» https://doi.org/10.1007/s10637-019-00823-2

Gehrcke M, Brum TB, Rosa LS, Ilha BD, Soares FZM, Cruz L. Incorporation of nanocapsules into gellan gum films: A strategy to improve the stability and prolong the cutaneous release of silibinin. Mater Sci Eng C 2021;119:111624. doi: 10.1016/j.msec.2020.111624

» https://doi.org/10.1016/j.msec.2020.111624

Gehrcke M, Giuliani LM, Ferreira LM, Barbieri AV, Marcondes MH, Silveira EF, et al. Enhanced photostability, radical scavenging and antitumor activity of indole-3-carbinol-loaded rose hip oil nanocapsules. Mater Sci Eng C 2017;74:279-286. doi: 10.1016/j.msec.2016.12.006

» https://doi.org/10.1016/j.msec.2016.12.006

He H, Ye J, Zhang X, Huang Y, Li X, Xiao M. κ-Carrageenan/locust bean gum as hard capsule gelling agents. Carbohydr Polym 2017;175:417-424. doi: 10.1016/j.carbpol.2017.07.049

» https://doi.org/10.1016/j.carbpol.2017.07.049

Jana S, Gandhi A, Sheet S, Sen KK. Metal ion-induced alginate-locust bean gum IPN microspheres for sustained oral delivery of aceclofenac. Int J Biol Macromol 2015; 72:47-53. doi: 10.1016/j.ijbiomac.2014.07.054

» https://doi.org/10.1016/j.ijbiomac.2014.07.054

Kaur R, Sharma A, Puri V, Singh I. Preparation and characterization of biocomposite films of carrageenan/locust bean gum/montmorrillonite for transdermal delivery of curcumin. BioImpacts 2019;9(1):37-43. doi: 10.15171/bi.2019.05

» https://doi.org/10.15171/bi.2019.05

Kim JK, Park SU. Current results on the biological and pharmacological activities of Indole-3-carbinol. EXCLI J 2018;17:181-185.

Kumar K, Dhawan N, Sharma H, Vaidya S, Vaidya B. Bioadhesive polymers: Novel tool for drug delivery. Artif Cells, Nanomed Biotechnol 2014;42(4):274-283. doi: 10.3109/21691401.2013.815194

» https://doi.org/10.3109/21691401.2013.815194

Mayba JN, Gooderham MJ. A guide to topical vehicle formulations. J Cutan Med Surg 2018;22(2):207-212. doi: 10.1177/1203475417743234

» https://doi.org/10.1177/1203475417743234

Meena LK, Raval P, Kedaria D, Vasita R. Study of locust bean gum reinforced cyst-chitosan and oxidized dextran based semi-IPN cryogel dressing for hemostatic application. Bioact Mater 2018; 3(3):370-384. doi: 10.1016/j.bioactmat.2017.11.005

» https://doi.org/10.1016/j.bioactmat.2017.11.005

Osmari BF, Giuliani LM, Reolon JB, Rigo GV, Tasca T, Cruz L. Gellan gum-based hydrogel containing nanocapsules for vaginal indole-3-carbinol delivery in trichomoniasis treatment. Eur J Pharm Sci 2020;151:105379. doi: 10.1016/j.ejps.2020.105379

» https://doi.org/10.1016/j.ejps.2020.105379

Pegoraro NS, Camponogara C, Gehrcke M, Giuliani LM, Silva DT, Maurer LH, et al. Oleic acid-containing semisolid dosage forms exhibit in vivo anti-inflammatory effect via glucocorticoid receptor in a UVB radiation-induced skin inflammation model. Inflammopharmacology 2020;28(3):773-786. doi: 10.1007/s10787-019-00675-5

» https://doi.org/10.1007/s10787-019-00675-5

Pettinelli N, Rodríguez-Llamazares S, Farrag Y, Bouza R, Barral L, Feijoo-Bandin S, et al. Poly(hydroxybutyrate-co-hydroxyvalerate) microparticles embedded in κ-carrageenan/locust bean gum hydrogel as a dual drug delivery carrier. Int J Biol Macromol 2020;146:110-118. doi: 10.1016/j.ijbiomac.2019.12.193

» https://doi.org/10.1016/j.ijbiomac.2019.12.193

Prado VC, Sari MHM, Borin BC, Pinheiro RC, Cruz L, Schuch A, et al. Development of a nanotechnological-based hydrogel containing a novel benzofuroazepine compound in association with vitamin E: An in vitro biological safety and photoprotective hydrogel. Colloids Surfaces B Biointerfaces 2021;199:111555. doi: 10.1016/j.colsurfb.2020.111555

» https://doi.org/10.1016/j.colsurfb.2020.111555

Rigo LA, Julia W, Silva CB, Beck RCR. Evaluation of the spreadability of pharmaceutical or cosmetic semisolid formulations using scanned images. Lat Am J Pharm 2012;31(10):1387-1391.

Rigon C, Marchiori MCL, Jardim FS, Peggoraro NS, Chaves PS, Velho MC, et al. Hydrogel containing silibinin nanocapsules presents effective anti-inflammatory action in a model of irritant contact dermatitis in mice. Eur J Pharm Sci 2019;137:104969. doi: 10.1016/j.ejps.2019.104969

» https://doi.org/10.1016/j.ejps.2019.104969

Saidin NM, Anuar NK, Meor Mohd Affandi MMR. Roles of polysaccharides in transdermal drug delivery system and future prospects. J Appl Pharm Sci 2018;8(3):141-157. doi: 10.7324/JAPS.2018.8320

» https://doi.org/10.7324/JAPS.2018.8320

Sari MHM, Fulco CWB, Ferreira LM, Pegoraro NS, Brum ES, Casola KK, et al. Nanoencapsulation potentiates the cutaneous anti-inflammatory effect of p,p′-methoxyl-diphenyl diselenide: Design, permeation, and in vivo studies of a nanotechnological-based carrageenan gum hydrogel. Eur J Pharm Sci 2020;153:105500. doi: 10.1016/j.ejps.2020.105500

» https://doi.org/10.1016/j.ejps.2020.105500

Sharadha M, Gowda DV, Vishal Gupta N, Akhila AR. An overview on topical drug delivery system - updated review. Int J Res Pharm Sci 2020;11(1):368-385. doi: 10.26452/ijrps.v11i1.1831

» https://doi.org/10.26452/ijrps.v11i1.1831

Teixeira MC, Severino P, Andreani T, Boonme P, Santini A, Silva AM, et al. D-α-tocopherol nanoemulsions: Size properties, rheological behavior, surface tension, osmolarity and cytotoxicity. Saudi Pharm J 2017;25(2):231-235. doi: 10.1016/j.jsps.2016.06.004

» https://doi.org/10.1016/j.jsps.2016.06.004

Timur SS, Yüksel S, Akca G, Şenel S. Localized drug delivery with mono and bilayered mucoadhesive films and wafers for oral mucosal infections. Int J Pharm 2019;559:102-112. doi: 10.1016/j.ijpharm.2019.01.029

» https://doi.org/10.1016/j.ijpharm.2019.01.029

Ullah F, Othman MBH, Javed F, Ahmad Z, Akil HM. Classification, processing and application of hydrogels: A review. Mater Sci Eng C 2015;57:414-433. doi: 10.1016/j.msec.2015.07.053

» https://doi.org/10.1016/j.msec.2015.07.053

Verma A, Tiwari A, Panda PK, Saraf S, Jain A, Jain SK. Locust Bean Gum in Drug Delivery Application Elsevier Inc.; 2019. doi: 10.1016/B978-0-12-817055-7.00008-X

» https://doi.org/10.1016/B978-0-12-817055-7.00008-X

Vijayaraghavan C, Vasanthakumar S, Ramakrishnan A. In vitro and in vivo evaluation of locust bean gum and chitosan combination as a carrier for buccal drug delivery. Pharmazie 2008;63(5):342-347. doi: 10.1691/ph.2008.7139

» https://doi.org/10.1691/ph.2008.7139

Yuan L, Pan M, Lei M, Zhou X, Hu D, Liu Q, et al. A novel composite of micelles and hydrogel for improving skin delivery of hydrocortisone and application in atopic dermatitis therapy. Appl Mater Today 2020;19:100593. doi: 10.1016/j.apmt.2020.100593

» https://doi.org/10.1016/j.apmt.2020.100593

Zepon KM, Martins MM, Marques MS, Heckler JM, Morisso FDP, Moreira MG, et al. Smart wound dressing based on κ-carrageenan/locust bean gum/cranberry extract for monitoring bacterial infections. Carbohydr Polym 2019;206(2018):362-370. doi: 10.1016/j.carbpol.2018.11.014

» https://doi.org/10.1016/j.carbpol.2018.11.014

Zhu BJ, Zayed MZ, Zhu HX, Zhao J, Li SP. Functional polysaccharides of carob fruit: A review. Chinese Med (United Kingdom) 2019;14(1):1-10. doi: 10.1186/s13020-019-0261-x

» https://doi.org/10.1186/s13020-019-0261-x

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Published

2023-06-13

Issue

Vol. 59 (2023)

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Original Article

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How to Cite

Locust bean gum hydrogels are bioadhesive and improve indole-3-carbinol cutaneous permeation: influence of the polysaccharide concentration. (2023). Brazilian Journal of Pharmaceutical Sciences, 59. https://doi.org/10.1590/s2175-97902023e21770

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