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Made available in DSpace on 2022-05-01T06:02:36Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-09-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Background: Although Curcumin (CUR) has great potential as a photosensitizer, the low solubility in water impairs its clinical performance in photodynamic inactivation (PDI). This study sought to establish an effective antimicrobial protocol for PDI using CUR in three different bioadhesive formulations. Methods: A CUR-loaded chitosan hydrogel with a poloxamer (CUR-CHIH), a CUR-loaded liquid crystal precursor system (CUR-LCP), a CUR-loaded microemulsion (CUR-ME), and CUR in dimethylsulfoxide (DMSO) solution (CUR-S; control formulation) were tested against in vitro and in situ oral biofilms. The optical properties of each formulation were evaluated. Results: All of the formulations exhibited lower absorbance than CUR-S; however, the CUR-LCP curve bore the highest resemblance. The CUR present in all formulations was completely degraded after 15 min of illumination. In vitro experiments showed that CUR-S was the only formulation able to significantly reduce biofilm viability of Candida albicans and Lactobacillus casei when compared to the negative control (no PDI); the amount of reduction obtained was 1.8 and 3.7 log (CFU/mL) for C. albicans and L. casei, respectively. There was a significant reduction on the viability of Streptococcus mutans biofilms when CUR-S and CUR-LCP were applied (approximately 3.5 and 1.6 log [CFU/mL], respectively). In situ testing showed antimicrobial efficacy against S. mutans and general microorganisms. Conclusions: Although the evaluated protocols has not been effective to all of the evaluated microorganisms, PDI showed potential against dental biofilms and evidence that the phototoxic effects of CUR have a high relation with the type of formulation in which it is loaded. Independent researcher at the moment of the submission (unaffiliated researcher) Department of Social Dentistry School of Dentistry UNESP - São Paulo State University Department of Clinical Analysis School of Pharmacy UNESP - São Paulo State University Department of Biosciences Piracicaba Dental School UNICAMP University of Campinas Department of Drugs and Pharmaceutics School of Pharmacy UNESP - São Paulo State University Department of Social Dentistry School of Dentistry UNESP - São Paulo State University Department of Clinical Analysis School of Pharmacy UNESP - São Paulo State University Department of Drugs and Pharmaceutics School of Pharmacy UNESP - São Paulo State University FAPESP: 2013/15770-6 FAPESP: 2015/24112-8

Curcumin-mediated Photodynamic Inactivation (PDI) has shown great potential to disinfect specific sites on tooth enamel but may involve contact with restorative materials. Thus, before use in dentistry, it is necessary to investigate whether the PDI protocol causes undesirable changes in the surfaces of aesthetic restorative materials and dental enamel. This study investigated the effect of PDI mediated by curcumin (CUR) in a liquid crystal precursor system on color stability (ΔE), surface roughness (Ra), and microhardness (kgf) of three different composite resins and bovine dental enamel specimens. The microhardness and roughness readings were performed 60 days after the treatments while the color readings were performed immediately, 24, 48, and 72 h, 7, 14, 21, 30, and 60 days after the treatments. Results showed that CUR mediated-PDI does not seem to have the potential to promote any esthetic or mechanical changes to the surface of tooth enamel and can be applied safely in clinical practice. However, the results on color, roughness, and hardness obtained for composite resins show that some negative effects can be produced, depending on the type of restorative material, more experiments must be performed with different formulations and, perhaps, with lower concentrations of CUR.

Made available in DSpace on 2022-05-01T08:44:42Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-08-01 Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) The present study reports the performance of the pigment hypericin (HYP)-loaded poloxamer-based mucoadhesive in situ gelling liquid crystalline precursor system (LCPS) for the treatment of vulvovaginal candidiasis (VVC) in mice. LCPS composed of 40% of ethoxylated and propoxylated cetyl alcohol, 30% of oleic acid and cholesterol (7:1), 30% of a dispersion of 16% poloxamer 407 and 0.05% of HYP (HYP-LCPS) was prepared and characterized by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS) and ex vivo permeation and retention studies across vaginal porcine mucosa were performed. In addition, the antifungal properties of the HYP-LCPS were evaluated in a murine in vivo model; for this, infected C57BL female mice groups were treated with both HYP in solution and HYP-LCPS, and after 6 days colony forming unit (CFU)/ml count was performed. PLM and SAXS confirmed that HYP-LCPS is a microemulsion situated in boundary transition region confirming its action as an LCPS. When in contact with simulated vaginal fluid, HYP-LCPS became rigid and exhibited maltase crosses and bragg peaks characteristics of lamellar phase. Ex vivo permeation and retention studies showed that HYP-LCPS provides a localized treatment on the superficial layers of porcine vaginal mucosa. HYP-LCPS induced a significant reduction in the number of CFU/ml in the mice; thus this formulation indicated it is as effective as a commercial dosage form. It was concluded that LCPS maintains the biological activity of HYP and provides an adequate drug delivery system for this lipophilic molecule at the vaginal mucosa, being a promising option in cases of VVC. São Paulo State University (UNESP) School of Pharmaceutical Sciences, Araraquara Department of Biosciences Piracicaba Dental School University of Campinas - UNICAMP, Piracicaba Paraíba State University Campina Grande São Paulo State University (UNESP) School of Pharmaceutical Sciences, Araraquara FAPESP: 16/11198-4 FAPESP: 2019/10261-2

Made available in DSpace on 2021-06-25T10:55:13Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-04-01. Added 1 bitstream(s) on 2021-07-15T15:05:25Z : No. of bitstreams: 1 S0103-50532021000400786.pdf: 944248 bytes, checksum: 167925933dc0ec4ec63ea2afbf080153 (MD5) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Platonia insignis fruit, popularly known as bacuri, is traditionally used in folk medicine for its anti-inflammatory and antioxidant properties. Therefore, this study determined the chemical composition and biological activities of the bacuri’s shell and seeds extracts, considered residues from its consumption and industrial uses. Four biflavonoids (GB-2a, GB-1a, morelloflavone, and volkensiflavone) were identified in the extracts by high-performance liquid chromatography-diode array detection (HPLC-DAD), liquid chromatography tandem mass spectrometry (LC-MS/MS), and liquid chromatography-solid phase extraction-nuclear magnetic resonance (LC-SPE-NMR) techniques. Morelloflavone was identified as the main compound in the shell ethyl acetate extract, being responsible for the high in vitro antioxidant (50% effective concentration (EC50) ranging from 8.0-10.5 µg mL−1 in different protocols), anti-glycant (80%), and moderate inhibition of nitric oxide (1.56 µg mL−1 for > 90% cell viability) activities. This extract showed promising in vivo anti-inflammatory activity evaluated through the paw edema protocol after its incorporation into a liquid-crystalline drug carrier system, reducing the edema by up to 31%. The results demonstrated the potential of the fruit for the development of drugs of natural origin and corroborated to add economic value to these discarded residues. Núcleo de Bioensaios Biossíntese e Ecofisiologia de Produtos Naturais (NuBBE) Departamento de Química Orgânica Instituto de Química Universidade Estadual Paulista “Júlio de Mesquita Filho” (Unesp) Departamento de Fármacos e Medicamentos Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista “Júlio de Mesquita Filho” (Unesp) Laboratório de Fitoquímica e Biomoléculas (LabFitoBio) Departamento de Química Universidade Estadual de Londrina (UEL) Faculdade de Ciências Exatas e Tecnologia (FACET) Universidade Federal da Grande Dourados (UFGD) Departamento de Genética e Morfologia Universidade de Brasília (UnB) Departamento de Ciências Biológicas Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista “Júlio de Mesquita Filho” (Unesp) Núcleo de Bioensaios Biossíntese e Ecofisiologia de Produtos Naturais (NuBBE) Departamento de Química Orgânica Instituto de Química Universidade Estadual Paulista “Júlio de Mesquita Filho” (Unesp) Departamento de Fármacos e Medicamentos Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista “Júlio de Mesquita Filho” (Unesp) Departamento de Ciências Biológicas Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista “Júlio de Mesquita Filho” (Unesp) CNPq: 142014/2018-4 CNPq: 159735/2017-3 FAPESP: 2013/07600-3 CNPq: 2014/465637-0 FAPESP: 2014/50926-0 FAPESP: 2016/16970-7 FAPESP: 2017/18807-9 FAPESP: 2017/19870-6

Made available in DSpace on 2021-06-25T15:00:53Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-03-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Cervical cancer is the fourth most common cancer in women. Conventional treatments involve surgery, radiotherapy and radiochemotherapy, which affect negatively the life quality. Bioactive molecules, such as curcumin (CUR), are potential alternatives for cervical cancer treatment. However, CUR has limited solubility in water, thus it is interesting to develop drug delivery systems to improve its clinical use. Here, we propose a liquid crystalline system (LCS) as a medium for the formulation and vaginal administration of CUR. To the best of our knowledge, this is the first study that showed the effect of vaginal mucus on the behavior of the liquid crystalline system as well as the antiangiogenic effect of curcumin incorporated in this system in the CAM model. We formulated LCS based on oleic acid, ethoxylated and propoxylated cetyl alcohol and aqueous phase containing water (FW) or dispersion of chitosan associated with polyethyleneimine (FPC). The characterization methodology revealed that LCS presented a lamellar mesophase, which remained stable in the presence of CUR and artificial vaginal mucus. Rheological, texture, and mucoadhesive tests showed that FPC demonstrated properties desirable for vaginal formulations. In vitro release and ex vivo permeation and retention validated the controlled-release properties of the system. LCS released approximately twice as much CUR as the control in 12 h, while ex-vivo porcine vaginal mucosa retained about 2.3% of CUR from LCS.These formulations revealed biocompatibility for L929 cells and toxicity for Hela cells. The vascular changes in response to this potential treatment were evaluated using the chick embryo chorioallantoic membrane (CAM) as a model. The caliber and the number of vessels reduced after the application of CUR-loaded formulations, encouraging the application of the mucoadhesive LCS developed for cervical cancer treatment. (C) 2020 Elsevier B.V. All rights reserved. Sao Paulo State Univ, Sch Pharmaceut Sci, Dept Drugs & Med, BR-01049010 Araraquara, SP, Brazil Univ Estadual Campinas, Piracicaba Dent Sch, Dept Biosci, BR-13414903 Piracicaba, SP, Brazil Univ Sao Paulo, Sao Carlos Inst Phys, BR-13560970 Sao Carlos, SP, Brazil Sao Paulo State Univ, Sch Pharmaceut Sci, Dept Drugs & Med, BR-01049010 Araraquara, SP, Brazil FAPESP: 2017/23357-2 FAPESP: 2019/07245-5 FAPESP: 2018/234304 FAPESP: 2016/14033-6

Made available in DSpace on 2021-06-25T12:42:33Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-02-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Programa de Apoio ao Desenvolvimento Cientifico (PADC) Current researches report an actual benefit of a treatment for oral cancer via inhibition of proteolytic matrix metalloproteinases (MPP) with a peptide drug, called CTT1. However, peptides present poor oral bioavailability. Topical administration on oral mucosa avoids its passage through the gastrointestinal tract and the first-pass liver metabolism, but the barrier function of the oral mucosa can impair the permeation and retention of CTT1. The objective of this study is to incorporate CTT1 into a mucoadhesive precursor of liquid crystalline system (PLCS) as an interesting strategy for the topical treatment of oral cancer. PLCS consisting of oleic acid, ethoxylated 20 and propoxylated cetyl alcohol 5, polyethyleneimine (P)-associated chitosan (C) dispersion and CTT1 (FPC-CTT1) was developed and characterized by polarized light microscopy (PLM) and small-angle X-ray scattering (SAXS). In vitro permeation and retention across esophageal mucosa, in vitro cytotoxicity towards tongue squamous cell carcinoma cells, and in vivo evaluation of vascular changes using the chick embryo chorioallantoic membrane (CAM) model were performed. PLM and SAXS showed that FPC-CTT1acted as PLCS, because it formed a lamellar liquid crystalline system after the addition of artificial saliva. FPC-CTT1increased approximately 2-fold the flux of permeation and 3- fold the retention of CTT1 on the porcine esophageal mucosa. CTT1 does not affect cell viability. CAM tests showed that FPC preserved the blood vessels and it can be a safe formulation. These findings encourage the use of the FPC-CTT1 for topical treatment of oral cancer. Univ Estadual Campinas, UNICAMP, Piracicaba Dent Sch Dept Biosci, BR-13414903 Piracicaba, SP, Brazil Sao Paulo State Univ, Sch Pharmaceut Sci, Dept Drugs & Med, UNESP, BR-14800903 Araraquara, SP, Brazil Univ Minho, Life & Hlth Sci Res Inst ICVS, Sch Hlth Sci, P-4710057 Braga, Portugal ICVS 3Bs PT Govt Associate Lab, P-4710057 Braga, Portugal Sao Paulo State Univ, Sch Pharmaceut Sci, Dept Drugs & Med, UNESP, BR-14800903 Araraquara, SP, Brazil FAPESP: 13/015651 FAPESP: 16/06337-5 FAPESP: 19/07245-5 FAPESP: 2014/50928-2 CNPq: 465687/2014-8

Made available in DSpace on 2019-10-06T17:13:40Z (GMT). No. of bitstreams: 0 Previous issue date: 2019-08-01 The vaginal mucosa is a very promising route for drug administration due to its high permeability and the possibility to bypass first pass metabolism; however, current vaginal dosage forms present low retention times due to their dilution in vaginal fluids, which hampers the efficacy of many pharmacological treatments. In order to overcome these problems, this study proposes to develop a mucoadhesive in situ gelling liquid crystalline precursor system composed of 30% of oleic acid and cholesterol (7:1), 40% of ethoxylated and propoxylated cetyl alcohol, and 30% of a dispersion of 16% Poloxamer 407. The effect of the dilution with simulated vaginal fluid (SVF) on this system was evaluated by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheological studies, texture profile analysis (TPA), mucoadhesion study, in vitro drug release test using hypericin (HYP) as drug model, and cytotoxicity assay. PLM and SAXS confirmed the formation of an isotropic system. After the addition of three different concentrations of SVF (30, 50, and 100%), the resultant formulations presented anisotropy and characteristics of viscous lamellar phases. Rheology shows that formulations with SVF behaved as a non-Newtonian fluid with suitable shear thinning for vaginal application. TPA and mucoadhesion assays indicated the formation of long-range ordered systems as the amount of SVF increases which may assist in the fixation of the formulation on the vaginal mucosa. The formulations were able to control about 75% of the released HYP demonstrating a sustained release profile. Finally, all formulations acted as safe vaginal drug delivery systems. School of Pharmaceutical Sciences São Paulo State University (UNESP) Paraíba State University Center for Natural Sciences and Humanities Federal University of ABC (UFABC) School of Pharmaceutical Sciences São Paulo State University (UNESP)

Bruno Fonseca-Santos,* Cínthia Yuka Satake,* Giovana Maria Fioramonti Calixto,* Aline Martins dos Santos, Marlus Chorilli School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, São Paulo, Brazil *These authors contributed equally tothis work Abstract: Resveratrol (Res) is a common phytoalexin present in a few edible materials, such as grape skin, peanuts, and red wine. Evidence has shown the beneficial effects of Res on human health, which may be attributed to its anti-inflammatory activity. However, the poor aqueous solubility of Res limits its therapeutic effectiveness. Therefore, the use of nanostructured delivery systems for Res, such as liquid-crystalline systems, could be beneficial. In this study, we aimed to develop, characterize, and determine the in vivo effectiveness of Res-loaded liquid-crystalline systems. Systems containing copaiba balsam oil, polyethylene glycol-40 hydrogenated castor oil, and water were designed. Results of polarized light microscopy, small-angle X-ray scattering, texture-profile analysis, and flow-rheology analysis showed that the Res-loaded liquid-crystalline system had a lamellar structure, textural and mechanical (hardness, compressibility, and adhesiveness) properties, and behaved as a non-Newtonian fluid, showing pseudoplastic behavior upon skin application. Furthermore, all liquid-crystalline systems presented bioadhesive properties that may have assisted in maintaining the anti-inflammatory activity of Res, since the topical application of the Res-loaded lamellar mesophase liquid crystals resulted in edema inhibition in a carrageenan-induced paw-inflammation mouse model. Therefore, Res-loaded lamellar mesophases represent a promising new therapeutic approach for inhibition of skin inflammation. Keywords: lamellar mesophase, liquid crystals, anti-inflammatory properties, topical delivery

Made available in DSpace on 2018-12-11T17:04:45Z (GMT). No. of bitstreams: 0 Previous issue date: 2016-05-20 Antimicrobial photodynamic therapy (aPDT) is increasingly being explored for treatment of periodontitis. Here, we investigated the effect of aPDT on human dental plaque bacteria in suspensions and biofilms in vitro using methylene blue (MB)-loaded poly(lactic-co-glycolic) (PLGA) nanoparticles (MB-NP) and red light at 660 nm. The effect of MB-NP-based aPDT was also evaluated in a clinical pilot study with 10 adult human subjects with chronic periodontitis. Dental plaque samples from human subjects were exposed to aPDT—in planktonic and biofilm phases—with MB or MB-NP (25 μ/mL) at 20 J/cm2 in vitro. Patients were treated either with ultrasonic scaling and scaling and root planing (US + SRP) or ultrasonic scaling + SRP + aPDT with MB-NP (25 μ/mL and 20 J/cm2) in a split-mouth design. In biofilms, MB-NP eliminated approximately 25% more bacteria than free MB. The clinical study demonstrated the safety of aPDT. Both groups showed similar improvements of clinical parameters one month following treatments. However, at three months ultrasonic SRP + aPDT showed a greater effect (28.82%) on gingival bleeding index (GBI) compared to ultrasonic SRP. The utilization of PLGA nanoparticles encapsulated with MB may be a promising adjunct in antimicrobial periodontal treatment. Faculdade de Ciencias Farmaceuticas UNESP—Univ Estadual Paulista Departamento de Análises Clínicas, Campus Araraquara Faculdade de Ciencias Farmaceuticas UNESP—Univ Estadual Paulista Departamento de Farmacos e Medicamentos, Campus Araraquara Instituto de Fisica de Sao Carlos Universidade de Sao Paulo, Caixa Postal 369 Applied Molecular Photomedicine Laboratory The Forsyth Institute, 245 First Street Department of PharmaceuticalSciences School of Pharmacy Bouvé College of Health Sciences Northeastern University, 140 The Fenway, Room 156, 360 Huntington Avenue Faculdade de Ciencias Farmaceuticas UNESP—Univ Estadual Paulista Departamento de Análises Clínicas, Campus Araraquara Faculdade de Ciencias Farmaceuticas UNESP—Univ Estadual Paulista Departamento de Farmacos e Medicamentos, Campus Araraquara

Made available in DSpace on 2018-12-11T17:28:17Z (GMT). No. of bitstreams: 0 Previous issue date: 2016-05-01 Tuberculosis (TB) is an infectious disease caused mainly by the bacillus Mycobacterium tuberculosis (Mtb), presenting 9.5 million new cases and 1.5 million deaths in 2014. The aim of this study was to evaluate a nanostructured lipid system (NLS) composed of 10% phase oil (cholesterol), 10% surfactant (soy phosphatidylcholine, sodium oleate), and Eumulgin® HRE 40 ([castor oil polyoxyl-40-hydrogenated] in a proportion of 3:6:8), and an 80% aqueous phase (phosphate buffer pH = 7.4) as a tactic to enhance the in vitro anti-Mtb activity of the copper(II) complexes [CuCl2(INH)2] H2O (1), [Cu(NCS)2(INH)2]5H2O (2) and [Cu(NCO)2(INH)2]4H2O (3). The Cu(II) complex-loaded NLS displayed sizes ranging from 169.5 ± 0.7095 to 211.1 ± 0.8963 nm, polydispersity index (PDI) varying from 0.135 ± 0.0130 to 0.236 ± 0.00100, and zeta potential ranging from -0.00690 ± 0.0896 to 8.43 ± 1.63 mV. Rheological analysis showed that the formulations behave as non-Newtonian fluids of the pseudoplastic and viscoelastic type. Antimycobacterial activities of the free complexes and NLS-loaded complexes against Mtb H37Rv ATCC 27294 were evaluated by the REMA methodology, and the selectivity index (SI) was calculated using the cytotoxicity index (IC50) against Vero (ATCC® CCL-81), J774A.1 (ATCC® TIB-67), and MRC-5 (ATCC® CCL-171) cell lines. The data suggest that the incorporation of the complexes into NLS improved the inhibitory action against Mtb by 52-, 27-, and 4.7-fold and the SI values by 173-, 43-, and 7-fold for the compounds 1, 2 and 3, respectively. The incorporation of the complexes 1, 2 and 3 into the NLS also resulted in a significant decrease of toxicity towards an alternative model (Artemia salina L.). These findings suggest that the NLS may be considered as a platform for incorporation of metallic complexes aimed at the treatment of TB. Faculdade de Ciencias Farmaceuticas UNESP—Univ Estadual Paulista, Campus Araraquara Instituto de Química UNESP—Univ Estadual Paulista, Campus Araraquara Faculdade de Ciencias Farmaceuticas UNESP—Univ Estadual Paulista, Campus Araraquara Instituto de Química UNESP—Univ Estadual Paulista, Campus Araraquara

Made available in DSpace on 2018-12-11T17:24:11Z (GMT). No. of bitstreams: 0 Previous issue date: 2016-02-18 Methotrexate (MTX) is an immunosuppressive drug for systemic use in the treatment of skin diseases, however, MTX presents a number of side effects, such as hepatotoxicity. To overcome this limitation, this study developed skin MTX delivery surfactant systems, such as a microemulsion (ME) and a liquid crystalline system (LCS), consisting of a glycol copolymer-based silicone fluid (SFGC) as oil phase, polyether functional siloxane (PFS) as surfactant, and carbomer homopolymer type A (C971) dispersion at 0.5% (wt/wt) as aqueous phase. Polarized light microscopy and small-angle X-ray scattering evidenced the presence of hexagonal and lamellar LCSs, and also a ME. Texture profile and in vitro bioadhesion assays showed that these formulations are suitable for topical application, showing interesting hardness, adhesiveness and compressibility values. Rheology analysis confirmed the Newtonian behaviour of the ME, whereas lamellar and hexagonal LCSs behave as pseudoplastic and dilatant non-Newtonian fluids, respectively. In vitro release profiles indicated that MTX could be released in a controlled manner from all the systems, and the Weibull model showed the highest adjusted coefficient of determination. Finally, the formulations were not cytotoxic to the immortalized human keratinocyte line HaCaT. Therefore, these bioadhesive surfactant systems established with PFS and C971 have great potential as skin delivery systems. Faculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP, 14800-850, Brazil Faculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP, 14800-850, Brazil. larissa_alvarenga@ymail.com Faculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Departamento de Análises Clínicas, Araraquara, SP 14800-850, Brazil Faculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP, 14800-850, Brazil. eliete.vz@gmail.com Faculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP, 14800-850, Brazil. pgremiao@fcfar.unesp.br

Made available in DSpace on 2018-12-11T17:30:23Z (GMT). No. of bitstreams: 0 Previous issue date: 2016-01-01 Decapeptide KSL-W shows antibacterial activities and can be used in the oral cavity, however, it is easily degraded in aqueous solution and eliminated. Therefore, we aimed to develop liquid crystalline systems (F1 and F2) for KSL-W buccal administration to treat multispecies oral biofilms. The systems were prepared with oleic acid, polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol (PPG-5-CETETH-20), and a 1% poloxamer 407 dispersion as the oil phase (OP), surfactant (S), and aqueous phase (AP), respectively. We characterized them using polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheology, and in vitro bioadhesion, and performed in vitro biological analysis. PLM showed isotropy (F1) or anisotropy with lamellar mesophases (F2), confirmed by peak ratio quantification using SAXS. Rheological tests demonstrated that F1 exhibited Newtonian behavior but not F2, which showed a structured AP concentration-dependent system. Bioadhesion studies revealed an AP concentration-dependent increase in the system's bioadhesiveness (F2 = 15.50 ±1.00 mN s) to bovine teeth blocks. Antimicrobial testing revealed 100% inhibition of multispecies oral biofilm growth after KSL-W administration, which was incorporated in the F2 aqueous phase at a concentration of 1 mg/mL. Our results suggest that this system could serve as a potential vehicle for buccal administration of antibiofilm peptides. School of Pharmaceutical Sciences Sao Paulo State University UNESP, Rodovia Araraquara-Jaú Km 01 Chemistry Institute UNESP Sao Paulo State University School of Pharmaceutical Sciences Sao Paulo State University UNESP, Rodovia Araraquara-Jaú Km 01 Chemistry Institute UNESP Sao Paulo State University