Salvado de harina y salvado de fécula de mandioca como potenciales excipientes para comprimidos

Acknowledgements: Fundação Dom Aguirre, for finantial support to Valéria Campos Orsi. Project funding by Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP, São Paulo, Brazil) (FAPESP Ref. No. 2018/05522-9 (Project PsaPhageKill)) in the form of a BPE fellowship granted to Victor M. Balcão is hereby gratefully acknowledged. This work also received support from CNPq, National Council for Scientific and Technological Development Brazil, in the form of Research Productivity (PQ) fellowships granted to Victor M. Balcão (Refs. No. 306113/2014-7 and 308208/2017-0).Objectives: The physicochemical characteristics of bran of cassava starch flour and bran of cassava flour (viz. organoleptic characteristics, pH value, moisture content, total ashes, lipid, protein, starch and fiber contents) and biopharmacotechnical parameters (viz. granulometry, flow capacity, angle at rest, outflow time and apparent density) were evaluated aiming at assessing their potential use as tablet excipients. Methodos: Three tablet formulations of venlafaxine hydrochloride were proposed, having as excipients bran of cassava flour, bran of cassava starch flour and Starch 1500®. The tablets were produced using two different pressures (98±5 MPa and 32±6 Mpa) and their mechanical (hardness and friability) and dissolubility characteristics were evaluated. Results and Conclusions: The tablets produced with both cassava flours, using higher pressures, presented similar physicochemical characteristics to those obtained with the excipient Starch1500®, thus indicating that cassava flours possess the potential to be used as disintegrating agents in tablets.Objetivos: Se evaluaron características físico-químicas del salvado de harina y del salvado de la fécula de mandioca (características organolépticas, pH, humedad, cenizas totales y contenido de lípidos, proteínas, almidones y fibras) y biofarmacotécnicas (granulometría, capacidad de flujo, ángulo en reposo, tiempo de salida y densidad aparente) con el objetivo de evaluar el uso de estos residuos como excipientes para comprimidos. Métodos: Se propusieron tres formulaciones en comprimidos de venlafaxina teniendo como excipientes salvado de harina de mandioca, salvado de fécula de mandioca y Starch 1500 ®. Las pastillas se produjeron utilizando dos presiones diferentes (98 ± 5 MPa y 32 ± 6 Mpa). Las características mecánicas (dureza y friabilidad) y de disolución de los comprimidos se evaluaron. Resultados y Conclusiones: Los comprimidos producidos con ambos salvados de mandioca, utilizando las presiones más elevadas, presentaron características físico-químicas similares a las obtenidas con el excipiente Starch1500®, indicando que las harinas de mandioca poseen potencial para ser utilizadas como agentes desintegrantes en comprimidos

Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate

ABSTRACT Azithromycin is a water-insoluble drug, with a very low bioavailability. In order to increase the solubility and dissolution rate, and consequently increase the bioavailability of poorly-soluble drugs (such as azithromycin), various techniques can be applied. One of such techniques is "solid dispersion". This technique is frequently used to improve the dissolution rate of poorly water-soluble compounds. Owing to its low solubility and dissolution rate, azithromycin does not have a suitable bioavailability. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of azithromycin by preparing its solid dispersion, using different Polyethylene glycols (PEG). Preparations of solid dispersions and physical mixtures of azithromycin were made using PEG 4000, 6000, 8000, 12000 and 20000 in various ratios, based on the solvent evaporation method. From the studied drug release profile, it was discovered that the dissolution rate of the physical mixture, as the well as the solid dispersions, were higher than those of the drug alone. There was no chemical incompatibility between the drug and polymer from the observed Infrared (IR) spectra. Drug-polymer interactions were also investigated using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD) and Scanning Election Microscopy (SEM). In conclusion, the dissolution rate and solubility of azithromycin were found to improve significantly, using hydrophilic carriers, especially PEG 6000

Development And Characterization Of A Cationic Lipid Nanocarrier As Non-viral Vector For Gene Therapy

The aim of the present work was to produce a cationic solid lipid nanoparticle (SLN) as non-viral vector for protein delivery. Cationic SLN were produced by double emulsion method, composed of softisan® 100, cetyltrimethylammonium bromide (CTAB), Tween® 80, Span® 80, glycerol and lipoid® S75 loading insulin as model protein. The formulation was characterized in terms of mean hydrodynamic diameter (z-ave), polydispersity index (PI), zeta potential (ZP), stability during storage time, stability after lyophilization, effect of toxicity and transfection ability in HeLa cells, in vitro release profile and morphology. SLN were stable for 30 days and showed minimal changes in their physicochemical properties after lyophilization. The particles exhibited a relatively slow release, spherical morphology and were able to transfect HeLa cells, but toxicity remained an obstacle. Results suggest that SLN are nevertheless promising for delivery of proteins or nucleic acids for gene therapy.667882Boulaiz, H., Marchal, J.A., Prados, J., Melguizo, C., Aranega, A., Non-viral and viral vectors for gene therapy (2005) Cell. Mol. Biol. (Noisy-le-grand), 51, pp. 3-22Bozelli, J.C., Jr., Sasahara, E.T., Pinto, M.R., Nakaie, C.R., Schreier, S., Effect of head group and curvature on binding of the antimicrobial peptide tritrpticin to lipid membranes (2012) Chem. Phys. Lipids, 165, pp. 365-373Bradford, M.M., Rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding (1976) Anal. Biochem., 72, pp. 248-254Brgles, M., Santak, M., Halassy, B., Forcic, D., Tomasic, J., Influence of charge ratio of liposome/DNA complexes on their size after extrusion and transfection efficiency (2012) Int. J. Nanomed., 7, pp. 393-401Carbone, C., Tomasello, B., Ruozi, B., Renis, M., Puglisi, G., Preparation and optimization of PIT solid lipid nanoparticles via statistical factorial design (2012) Eur. J. Med. Chem., 49, pp. 110-117Carbone, C., Campisi, A., Manno, D., Serra, A., Spatuzza, M., Musumeci, T., Bonfanti, R., Puglisi, G., The critical role of didodecyldimethylammonium bromide on physico-chemical, technological and biological properties of NLC (2014) Colloids Surf. B Biointerfaces, 121, pp. 1-10Carbone, C., Campisi, A., Musumeci, T., Raciti, G., Bonfanti, R., Puglisi, G., FA-loaded lipid drug delivery systems: Preparation, characterization and biological studies (2014) Eur. J. Pharm. Sci., 52, pp. 12-20Choi, W.J., Kim, J.K., Choi, S.H., Park, J.S., Ahn, W.S., Kim, C.K., Low toxicity of cationic lipid-based emulsion for gene transfer (2004) Biomaterials, 25, pp. 5893-5903Choi, S.H., Jin, S.E., Lee, M.K., Lim, S.J., Park, J.S., Kim, B.G., Ahn, W.S., Kim, C.K., Novel cationic solid lipid nanoparticles enhanced p53 gene transfer to lung cancer cells (2008) Eur. J. Pharm. Biopharm., 68, pp. 545-554Cortesi, R., Bergamini, P., Ravani, L., Drechsler, M., Costenaro, A., Pinotti, M., Campioni, M., Esposito, E., Long-chain cationic derivatives of PTA (1,3,5-triaza-7-phosphaadamantane) as new components of potential non-viral vectors (2012) Int. J. Pharm., 431, pp. 176-182Del Pozo-Rodriguez, A., Delgado, D., Solinis, M.A., Gascon, A.R., Pedraz, J.L., Solid lipid nanoparticles: Formulation factors affecting cell transfection capacity (2007) Int. J. Pharm., 339, pp. 261-268Doktorovova, S., Shegokar, R., Rakovsky, E., Gonzalez-Mira, E., Lopes, C.M., Silva, A.M., Martins-Lopes, P., Souto, E.B., Cationic solid lipid nanoparticles (cSLN): Structure, stability and DNA binding capacity correlation studies (2011) Int. J. Pharm., 420, pp. 341-349Doktorovova, S., Shegokar, R., Martins-Lopes, P., Silva, A.M., Lopes, C.M., Muller, R.H., Souto, E.B., Modified Rose Bengal assay for surface hydrophobicity evaluation of cationic solid lipid nanoparticles (cSLN) (2012) Eur. J. Pharm. Sci., 45, pp. 606-612Fangueiro, J.F., Andreani, T., Egea, M.A., Garcia, M.L., Souto, S.B., Silva, A.M., Souto, E.B., Design of cationic lipid nanoparticles for ocular delivery: Development, characterization and cytotoxicity (2014) Int. J. Pharm., 461, pp. 64-73Griffin, W.C., Classification of surface active agents by HLB (1949) J. Soc. Cosmet. Chem., 1, pp. 311-326Griffin, W.C., Calculation of HLB valuess of nonionic surfactants (1954) J. Soc. Cosmet. Chem., 5, pp. 249-256Howard, M.D., Lu, X., Jay, M., Dziubla, T.D., Optimization of the lyophilization process for long-term stability of solid-lipid nanoparticles (2012) Drug Dev. Ind. Pharm.Hwang, T.L., Sung, C.T., Aljuffali, I.A., Chang, Y.T., Fang, J.Y., Cationic surfactants in the form of nanoparticles and micelles elicit different human neutrophil responses: A toxicological study (2014) Colloids Surf. B Biointerfaces, 114, pp. 334-341Jiang, Z., Sun, C., Yin, Z., Zhou, F., Ge, L., Liu, X., Kong, F., Comparison of two kinds of nanomedicine for targeted gene therapy: Premodified or postmodified gene delivery systems (2012) Int. J. Nanomed., 7, pp. 2019-2031Juillerat-Jeanneret, L., Schmitt, F., Chemical modification of therapeutic drugs or drug vector systems to achieve targeted therapy: Looking for the grail (2007) Med. Res. Rev., 27, pp. 574-590Liu, C.H., Yu, S.Y., Cationic nanoemulsions as non-viral vectors for plasmid DNA delivery (2010) Colloids Surf. B Biointerfaces, 79, pp. 509-515Liu, C.H., Yu, S.Y., Cationic nanoemulsions as non-viral vectors for plasmid DNA delivery (2012) Colloids Surf. B Biointerfaces, 79, pp. 509-515Liu, Z., Zhong, Z., Peng, G., Wang, S., Du, X., Yan, D., Zhang, Z., Liu, J., Folate receptor mediated intracellular gene delivery using the charge changing solid lipid nanoparticles (2009) Drug Deliv., 16, pp. 341-347Olbrich, C., Bakowsky, U., Lehr, C.M., Muller, R.H., Kneuer, C., Cationic solid-lipid nanoparticles can efficiently bind and transfect plasmid DNA (2001) J. Control Release, 77, pp. 345-355Radomska-Soukharev, A., Stability of lipid excipients in solid lipid nanoparticles (2007) Adv. Drug Deliv. Rev., 59, pp. 411-418Rudolph, C., Rosenecker, J., Formation of solid lipid nanoparticle (sln)-gene vector complexe for transfection of mammalian cells in vitro (2012) Cold Spring Harb Protoc, 2012 (3), pp. 357-360Severino, P., Souto, E.B., Pinho, S.C., Santana, M.H., Hydrophilic coating of mitotane-loaded lipid nanoparticles: Preliminary studies for mucosal adhesion (2013) Pharm. Dev. Technol., 18 (3), pp. 577-581. , Epub 2011 Sep 29Severino, P., Santana, M.H., Souto, E.B., Optimizing SLN and NLC by 22 full factorial design: Effect of homogenization technique (2012) Mater. Sci. Eng. C, 32, pp. 1375-1379Siddiqui, A., Gupta, V., Liu, Y.Y., Nazzal, S., Doxorubicin and MBO-asGCS oligonucleotide loaded lipid nanoparticles overcome multidrug resistance in adriamycin resistant ovarian cancer cells (NCI/ADR-RES) (2012) Int. J. Pharm., 431, pp. 222-229Siddiqui, A., Alayoubi, A., Nazzal, S., The effect of emulsifying wax on the physical properties of CTAB-based solid lipid nanoparticles (SLN) (2014) Pharm. Dev. Technol., 19, pp. 125-128Simberg, D., Weisman, S., Talmon, Y., Barenholz, Y., DOTAP (and other cationic lipids): Chemistry, biophysics, and transfection (2004) Crit. Rev. Ther. Drug Carrier Syst., 21, pp. 257-317Tabatt, K., Sameti, M., Olbrich, C., Muller, R.H., Lehr, C.M., Effect of cationic lipid and matrix lipid composition on solid lipid nanoparticle-mediated gene transfer (2004) Eur. J. Pharm. Biopharm., 57, pp. 155-162Tabatt, K., Sameti, M., Olbrich, C., Muller, R.H., Lehr, C.M., Effect of cationic lipid and matrix lipid composition on solid lipid nanoparticle-mediated gene transfer (2004) Eur. J. Pharm. Biopharm., 57, pp. 155-162Taveira, S.F., Araujo, L.M., De Santana, D.C., Nomizo, A., De Freitas, L.A., Lopez, R.F., Development of cationic solid lipid nanoparticles with factorial design-based studies for topical administration of doxorubicin (2012) J. Biomed. Nanotechnol., 8, pp. 219-228Toledo, M.A., Janissen, R., Favaro, M.T., Cotta, M.A., Monteiro, G.A., Prazeres, D.M., Souza, A.P., Azzoni, A.R., Development of a recombinant fusion protein based on the dynein light chain LC8 for non-viral gene delivery (2012) J. Control Release, 159, pp. 222-231Torchilin, V.P., Multifunctional nanocarriers (2006) Adv. Drug Deliv. Rev., 58, pp. 1532-1555Vighi, E., Ruozi, B., Montanari, M., Battini, R., Leo, E., PDNA condensation capacity and in vitro gene delivery properties of cationic solid lipid nanoparticles (2010) Int. J. Pharm., 389, pp. 254-261Vighi, E., Montanari, M., Ruozi, B., Iannuccelli, V., Leo, E., The role of protamine amount in the transfection performance of cationic SLN designed as a gene nanocarrier (2012) Drug Deliv., 19, pp. 1-10Wang, Y., Zhu, L., Dong, Z., Xie, S., Chen, X., Lu, M., Wang, X., Zhou, W., Preparation and stability study of norfloxacin-loaded solid lipid nanoparticle suspensions (2012) Colloids Surf. B Biointerfaces, 98, pp. 105-111Yang, T., Sheng, H.H., Feng, N.P., Wei, H., Wang, Z.T., Wang, C.H., Preparation of andrographolide-loaded solid lipid nanoparticles and their in vitro and in vivo evaluations: Characteristics, release, absorption, transports, pharmacokinetics, and antihyperlipidemic activity (2013) J. Pharm. Sci., 102, pp. 4414-4425Yu, W., Liu, C., Ye, J., Zou, W., Zhang, N., Xu, W., Novel cationic SLN containing a synthesized single-tailed lipid as a modifier for gene delivery (2009) Nanotechnology, 20, p. 21510

Solid Lipid Nanoparticles For Hydrophilic Biotech Drugs: Optimization And Cell Viability Studies (caco-2 & Hepg-2 Cell Lines)

Insulin was used as model protein to developed innovative Solid Lipid Nanoparticles (SLNs) for the delivery of hydrophilic biotech drugs, with potential use in medicinal chemistry. SLNs were prepared by double emulsion with the purpose of promoting stability and enhancing the protein bioavailability. Softisan®100 was selected as solid lipid matrix. The surfactants (Tween®80, Span®80 and Lipoid®S75) and insulin were chosen applying a 22 factorial design with triplicate of central point, evaluating the influence of dependents variables as polydispersity index (PI), mean particle size (z-AVE), zeta potential (ZP) and encapsulation efficiency (EE) by factorial design using the ANOVA test. Therefore, thermodynamic stability, polymorphism and matrix crystallinity were checked by Differential Scanning Calorimetry (DSC) and Wide Angle X-ray Diffraction (WAXD), whereas the effect of toxicity of SLNs was check in HepG2 and Caco-2 cells. Results showed a mean particle size (z-AVE) width between 294.6 nm and 627.0 nm, a PI in the range of 0.425-0.750, ZP about -3 mV, and the EE between 38.39% and 81.20%. After tempering the bulk lipid (mimicking the end process of production), the lipid showed amorphous characteristics, with a melting point of ca. 30 °C. The toxicity of SLNs was evaluated in two distinct cell lines (HEPG-2 and Caco-2), showing to be dependent on the concentration of particles in HEPG-2 cells, while no toxicity in was reported in Caco-2 cells. SLNs were stable for 24 h in in vitro human serum albumin (HSA) solution. The resulting SLNs fabricated by double emulsion may provide a promising approach for administration of protein therapeutics and antigens. © 2014 Published by Elsevier Masson SAS.812834FCT; Office of Fuel Cycle TechnologiesYang, R., Preparation of gel-core-solid lipid nanoparticle: A novel way to improve the encapsulation of protein and peptide (2010) Chem Pharm. Bull. (Tokyo), 58 (9), pp. 1195-1202Wong, H.L., Wu, X.Y., Bendayan, R., Nanotechnological advances for the delivery of CNS therapeutics (2011) Adv. Drug Deliv. Rev., 64 (7), pp. 686-700Carbone, C., Preparation and optimization of PIT solid lipid nanoparticles via statistical factorial design (2012) Eur. J. Med. Chem., 49, pp. 110-117Fonte, P., Chitosan-coated solid lipid nanoparticles for insulin delivery (2012) Methods Enzymol, 508, pp. 295-314Fangueiro, J.F., A novel lipid nanocarrier for insulin delivery: Production, characterization and toxicity testing Pharm. Dev. Technol.Sarmento, B., Oral insulin delivery by means of solid lipid nanoparticles (2007) Int. J. Nanomedicine, 2 (4), pp. 743-749Gallarate, M., Preparation of solid lipid nanoparticles from W/O/W emulsions: Preliminary studies on insulin encapsulation (2009) J. Microencapsul., 25 (5), pp. 394-402Doktorovova, S., Cationic solid lipid nanoparticles (cSLN): Structure, stability and DNA binding capacity correlation studies (2011) Int. J. Pharm., 420 (2), pp. 341-349Xie, S., Solid lipid nanoparticle suspension enhanced the therapeutic efficacy of praziquantel against tapeworm (2011) Int. J. Nanomedicine, 6, pp. 2367-2374Soares, S., Effect of freeze-drying, cryoprotectants and storage conditions on the stability of secondary structure of insulin-loaded solid lipid nanoparticles (2013) Int. J. Pharm., 18 (456), pp. 370-381Kabanov, A.V., Gendelman, H.E., Nanomedicine in the diagnosis and therapy of neurodegenerative disorders (2007) Progress in Polymer Science (Oxford), 32 (8-9), pp. 1054-1082. , DOI 10.1016/j.progpolymsci.2007.05.014, PII S0079670007000743, Polymers in Biomedical ApplicationsYassin, A.E., Optimization of 5-flurouracil solid-lipid nanoparticles: A preliminary study to treat colon cancer (2010) Int. J. Med. Sci., 7 (6), pp. 398-408Gaba, B., Nanostructured lipid (NLCs) carriers as a bioavailability enhancement tool for oral administration (2014) Drug Deliv., , 10.3109/10717544.2014.898110 (in press)Yang, R., Preparation of gel-core-solid lipid nanoparticle: A novel way to improve the encapsulation of protein and peptide (2010) Chem. Pharm. Bull., 58 (9), pp. 1195-1202Severino, P., Santana, M.H., Optimizing SLN and NLC by 2(2) full factorial design: Effect of homogenization technique (2012) Mater. Sci. Eng. C Mater. Biol. Appl., 32 (6), pp. 1375-1379Chen, C., Orally delivered salmon calcitonin-loaded solid lipid nanoparticles prepared by micelle-double emulsion method via the combined use of different solid lipids (2013) Nanomedicine, 8 (7), pp. 1085-1100Mojahedian, M.M., A novel method to produce solid lipid nanoparticles using n-butanol as an additional co-surfactant according to the o/w microemulsion quenching technique (2013) Chem. Phys. Lipids, 174, pp. 32-38Varshosaz, J., Comparing different sterol containing solid lipid nanoparticles for targeted delivery of quercetin in hepatocellular carcinoma (2013) J. Liposome Res., , 10.3109/08982104.2013.868476 (in press)Schmidts, T., Influence of hydrophilic surfactants on the properties of multiple w/o/w emulsions (2009) J. Colloid. Interface Sci., 338 (1), pp. 184-192Egorova, E.M., The validity of the Smoluchowski equation in electrophoretic studies of lipid membranes (1994) Electrophoresis, 15 (8-9), pp. 1125-1131Bradford, M.M., A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding (1976) Anal. Biochem., 72, pp. 248-254De Ven, H.V., Solid lipid nanoparticle (SLN) formulations as a potential tool for the reduction of cytotoxicity of saponins (2009) Die Pharmazie, 64 (3), pp. 172-176Hamid, R., Rotshteyn, Y., Rabadi, L., Parikh, R., Bullock, P., Comparison of alamar blue and MTT assays for high through-put screening (2004) Toxicology in Vitro, 18 (5), pp. 703-710. , DOI 10.1016/j.tiv.2004.03.012, PII S0887233304000633O'Brien, J., Investigation of the Alamar Blue (resazurin) fluorescent dye for the assessment of mammalian cell cytotoxicity (2000) Eur. J. Biochem., 267 (17), pp. 5421-5426Štěpánek, P., Static and dynamic properties of multiple light scattering (1993) J. Chem. Phys., 99, pp. 6384J-6393JStepanek, P., (1993) Dynamic light scattering. The method and some applications, , W. Brown, Oxford University Press New York 177, 2Štěpánek, P., Koňák, C., (1984) Adv. Colloid. Interface Sci., 21, pp. 195-274Severino, P., Polymorphism, crystallinity and hydrophilic-lipophilic balance of stearic acid and stearic acid-capric/caprylic triglyceride matrices for production of stable nanoparticles (2011) Colloid. Surf. B Biointerface, 86 (1), pp. 125-130Severino, P., Crystallinity of Dynasan®114 and Dynasan ®118 matrices for the production of stable Miglyol ®-loaded nanoparticles (2011) J. Therm. Anal. Calorim., 108, pp. 101-108Naruhashi, K., Comparison of the expression and function of ATP binding cassette transporters in Caco-2 and T84 cells on stimulation by selected endogenous compounds and xenobiotics (2011) Drug Metab. Pharmacokinet., 26 (2), pp. 145-153Bhattacharjee, S., Van Opstal, E.J., Alink, G.M., Marcelis, A.T.M., Zuilhof, H., Rietjens, I.M.C.M., Surface charge-specific interactions between polymer nanoparticles and ABC transporters in Caco-2 cells (2013) J. Nanoparticle Res., 15, p. 1695Doktorovova, S., Souto, E.B., Silva, A.M., Nanotoxicology applied to solid lipid nanoparticles and nanostructured lipid carriers - A systematic review of in vitro data (2014) Eur. J. Pharm. Biopharm., , 10.1016/j.ejpb.2014.02.005 (in press)Peters, (1996) In all about albumins: Biochemistry, genetics and medical applications, , Academic Press San DiegoGoppert, T.M., Muller, R.H., Plasma protein adsorption of tween 80- and poloxamer 188-stabilized solid lipid nanoparticles (2003) Journal of Drug Targeting, 11 (4), pp. 225-231. , DOI 10.1080/1061186031000161595

Nanostructured Lipid Carriers As A Strategy To Improve The In Vitro Schistosomiasis Activity Of Praziquantel

Praziquantel (PZQ) is a pyrazinoisoquinoline anthelmintic that was discovered in 1972 by Bayer Germany. Currently, due to its efficacy, PZQ is the drug of choice against all species of Schistosoma. Although widely used, PZQ exhibits low and erratic bioavailability because of its poor water solubility. Nanostructured lipid carriers (NLC), second-generation solid lipid nanoparticles, were developed in the 1990s to improve the bioavailability of poorly water soluble drugs. The aim of this study was to investigate nanostructured lipid carriers as a strategy to improve the efficacy of PZQ in S. mansoni treatment. We prepared NLC2 and NLC4 by adding seventy percent glycerol monostearate (GMS) as the solid lipid, 30% oleic acid (OA) as the liquid lipid and two surfactant systems containing either soybean phosphatidylcholine/poloxamer (PC/P-407) or phosphatidylcholine/Tween 60 (PC/T60), respectively. The carriers were characterized by nuclear magnetic resonance, differential scanning calorimetry, thermogravimetric analysis and Fourier transform-infrared spectroscopy. The safety profile was evaluated using red cell hemolysis and in vitro cytotoxicity assays. The results showed that the encapsulation of PZQ in NLC2 or NLC4 improved the safety profile of the drug. Treatment efficacy was evaluated on the S. mansoni BH strain. PZQ-NLC2 and PZQ-NLC4 demonstrated an improved efficacy in comparison with free PZQ. The results showed that the intestinal transport of free PZQ and PZQ-NLC2 was similar. However, we observed that the concentration of PZQ absorbed was smaller when PZQ was loaded in NLC4. The difference between the amounts of absorbed PZQ could indicate that the presence of T60 in the nanoparticles (NLC4) increased the rigid lipid matrix, prolonging release of the drug. Both systems showed considerable in vitro activity against S. mansoni, suggesting that these systems may be a promising platform for the administration of PZQ for treating schistosomiasis.151761772Barsoum, R.S., Esmat, G., El-Baz, T., (2013) Journal of Advanced Research, 4, p. 433De Oliveira, R.N., Rehder, V.L.G., Santos Oliveira, A.S., Júnior, Í.M., De Carvalho, J.E., De Ruiz, A.L.T.G., De Lourdes Sierpe Jeraldo, V., Allegretti, S.M., (2012) Experimental Parasitology, 132, p. 135Allegretti, S.M., Oliveira, C.N.F., Oliveira, R.N., Frezza, T.F., Rehder, V.L.G., (2012), 27. , www.intechopen.com/books/schistosomiasisBygott, J.M., Chiodini, P.L., (2009) Acta Tropica, 111, p. 95Zhang, S.-M., Coultas, K.A., (2013) International Journal for Parasitology: Drugs and Drug Resistance, 3, p. 28Gryseels, B., Polman, K., Clerinx, J., Kestens, L., (2006) The Lancet, 368, p. 1106Doenhoff, M.J., Cioli, D., Utzinger, J., (2008) Curr. Opin. Infect. Dis., 1, p. 659Stelma, F.F., Talla, I., Sow, S., Kongs, A., Niang, M., Polman, K., Deelder, A.M., Gryseels, B., (1995) Am. J. Trop. Med. Hyg., 53, p. 167Mourao, S.C., Costa, P.I., Salgado, H.R., Gremiao, M.P., (2005) Int. J. Pharm., 295, p. 157Frezza, T.F., Madi, R.R., Banin, T.M., Pinto, M.C., Souza, A.L.R., Gremião, M.P.D., Allegretti, S.M., (2007) Journal of Basic and Applied Pharmaceutical Sciences, 28, p. 209Yang, L., Geng, Y., Li, H., Zhang, Y., You, J., Chang, Y., (2009) Pharmazie, 64, p. 86Souza, A., Andreani, T., Nunes, F., Cassimiro, D., Almeida, A., Ribeiro, C., Sarmento, V., Souto, E., (2012) J. Therm. Anal. Calorim., 108, p. 353Almeida, A., Souza, A., Cassimiro, D., Gremião, M., Ribeiro, C., Crespi, M., (2012) J. Therm. Anal. Calorim., 108, p. 333Souza, A.L.R., Kiill, C.P., Santos, F.K., Luz, G.M., Silva, H.R., Chorilli, M., Gremião, M.P.D., (2012) Current Nanoscience, 8, p. 512Santos, F.K., Oyafuso, M.H., Kiill, C.P., Gremiao, M.P.D., Chorilli, M., (2013) Current Nanoscience, 9, p. 159Cinto, P., Souza, A., Lima, A., Chaud, M., Gremião, M., (2009) Chromatographia, 69, p. 213Frezza, T.F., Gremião, M.P.D., Zanotti-magalhães, E.M., Magalhães, L.A., Souza, A.L.R., Allegretti, S.M., (2013) Acta TropicaCampos, F.D.S., Cassimiro, D.L., Crespi, M.S., Almeida, A.E., Gremião, M.P.D., (2013) Brazilian Journal of Pharmaceutical Sciences, 49, p. 75Müller, R.H., Petersen, R.D., Hommoss, A., Pardeike, J., (2007) Advanced Drug Delivery Reviews, 59, p. 522Han, F., Li, S., Yin, R., Liu, H., Xu, L., (2008) Colloids Surf., A: Physicochemical and Engineering Aspects, 315, p. 210Martins, S., Silva, A.C., Ferreira, D.C., Souto, E.B., (2009) Journal Biomedical Nanotechnology, 5, p. 76Silva, A.C., Santos, D., Ferreira, D.C., Souto, E.B., (2009) Pharmazie, 64, p. 177Jumaa, M., Kleinebudde, P., Müller, B.W., (1999) Pharmaceutica Acta Helvetiae, 73, p. 293Huang, Z.R., Hua, S.C., Yang, Y.L., Fang, J.Y., (2008) Acta Pharmacol. Sin., 29, p. 1094Olivier, L., Stirewalt, M.A., (1952) The Journal of Parasitology, 38, p. 19Smithers, S.R., Terry, R.J., (1965) Parasitology, 55, p. 695Xiao, S.H., Keiser, J., Chollet, J., Utzinger, J., Dong, Y., Endriss, Y., Vennerstrom, J.L., Tanner, M., (2007) Antimicrob. Agents Chemother., 51, p. 1440Cassimiro, D.L., Ferreira, L.M.B., Capela, J.M.V., Crespi, M.S., Ribeiro, C.A., (2013) Journal Of Pharmaceutical and Biomedical Analysis, 73, p. 24Garnero, C., Zoppi, A., Genovese, D., Longhi, M., (2010) Carbohydrate Research, 345, p. 2550Bottom, R., (2008) Thermogravimetric Analysis, Principles and Applications of Thermal Analysis, p. 87. , Blackwell Publishing LtdJores, K., Mehnert, W., Mader, K., (2003) Pharm. Res., 20, p. 1274Ali, H., El-Sayed, K., Sylvester, P.W., Nazzal, S., (2010) Colloids Surf. B Biointerfaces, 77, p. 286Pople, P.V., Singh, K.K., (2011) Eur. J. Pharm. Biopharm., 79, p. 82De Jesus, M.B., Pinto, L.M.A., Fraceto, L.F., Takahata, L.A.Y., Jaime, P.E.C., (2006) J. Pharm. Biomed. Anal., 41, p. 1428Hi, E.-S., Aa, A.-B., (1998) Analytical Profiles of Drug Substances and Excipients, 25, p. 463Schepmann, D., Blaschke, G., (2001) J. Pharm. Biomed. Anal., 26, p. 791Malheiros, S.V.P., Meirelles, N.C., De Paula, E., (2000) Biophys. Chem., 83, p. 89Raina, N., Goyal, A.K., Pillai, C.R., Rath, G., (2013) Indian Journal of Pharmaceutical Education and Research, 47, p. 123Abbasalipourkabir, R., Salehzadeh, A., Abdullah, R., (2011) Biotechnology, 10, p. 528Chiann, C., Gonçalves, J.E., Gai, M.N.M.N., Storpirtis, S.S., (2009) Biofarmacotécnica, 1, p. 352. , Guanabara Koogan, São PauloBaldrick, P., (2000) Regulatory Toxicology and Pharmacology, 32, p. 210Custodio, J.M., Wu, C.Y., Benet, L.Z., (2008) Advanced Drug Delivery Reviews, 60, p. 717Disch, J., Katz, N., Pereira E Silva, Y., De Gouvea Viana, L., Andrade, M.O., Rabello, A., (2002) Acta Trop, 81, p. 133Cioli, D., Pica-Mattoccia, L., (2003) Parasitol. Res., 90, p. 22Oliveira, C.N.F.D., Oliveira, R.N.D., Frezza, T.F., Rehder, V.L.C.G., Allegretti, S.M., (2013) Tegument of Schistosoma Mansoni as A Therapeutic Target, Parasitic Diseases-SchistosomiasisVan Hellemond, J.J., Retra, K., Brouwers, J.F., Van Balkom, B.W., Yazdanbakhsh, M., Shoemaker, C.B., Tielens, A.G., (2006) Int. J. Parasitol., 36, p. 691Barth, L.R., Fernandes, A.P., Rodrigues, V., (1996) Rev. Inst. Med. Trop. Sao Paulo, 38, p. 423Wilson, T.H., Wiseman, G., (1954) J. Physiol., 123, p. 116Balimane, P.V., Chong, S., Morrison, R.A., (2000) J. Pharmacol. Toxicol. Methods, 44, p. 30