contributos para uma melhor qualidade de vida

Transcrição

1 Nutracêuticos, Libertação Controlada: contributos para uma melhor qualidade de vida Catarina Duarte

2 World USA Europe Source: Population Division, DESA, United Nations: World Population Ageing

3 Cumulative probabilities of reaching a proportion 60+ of one-third or more for the world and selected world regions by calendar year; in Nature 451, (7 February 2008).

4 Source: Population Division, DESA, United Nations: World Population Ageing

5 Increase in life expectancy Desire for an improved quality of life Population more awareof the benefits to health of the products they consume NATURAL INGREDIENTS Identification/Isolation and bioactivity studies (health promotion, prevention of diseases)

6 NATURAL INGREDIENTS Carotenoids, Fibers, Fatty Acids, FlavonoidsMinerals, Phenolic Acids, Sterols, Polyphenols, Phytoestrogens, Vitamins, Cosmeceuticals Pharmaceutical Industry Nutraceuticals Functional Food Cosmetic Industry Food Industry Nutricosmetics

7 Functional Foods foods that contain potentially bioactive products that may provide a health benefit beyond basic nutrition. Natural Food Enriched Food

8 Nutraceutical nutrition + pharmaceutical = NUTRACEUTICAL product isolated from foods or food derivatives, Generally, demonstrated to have a physiological benefit in the prevention and/ortreatment of disease and/or disorder sold in medicinal forms

9 Cosmeceutical Cosmeceuticals may contain active ingredients such as vitamins, phytochemicals, enzymes, antioxidants, and essential oils. The cosmeceutical label applies only to products applied topically, such as creams, lotions and ointments.

10 Nutricosmetics The big difference is that these products are taken orally to improve health and beauty,and according to the latest market study, it is a rapidly-growing category that is about to hit the major world markets. Nutricosmetic productshave mainly targeted the anti-ageingand haircare industries, with L'Oreal and Nestle joining together to create the products Imedeen, a skin care supplement, and Inneov, a skin care and hair care supplement.

11 Production of natural extracts from several botanical sources Mediterrean Diet (vegetables, fruit, fish, olive oil, wine) Clean Technology Residues and subproducts from food industry

12 Development of bioactivity assays to test health benefits Antioxidant evaluation LDL Oxidation Cellular Oxidative Stress Cytotoxicity Antiproliferative tests Anti-inflammatory inflammatory assays

13 Global Antioxidant Evaluation MF BE PPipo RP MS Fj S G GG Bravo de Esmolfe (BE) Malápio Fino (MF) Malápio da Serra (MS) Pêro Pipo (PP) Golden (G) Starking (S) Fuji (Fj) Gala Galaxy (GG) Reineta Parda (RP)

14 HO Intracelular Antioxidant Capacity H 2 O 2 Células Caco t-bhp RO ROO 15 Apple extract (100mg/mL) MF BE S MS PP FJ G GG RP 0 BE MF MS GG FJ RP S PP G BE MF MS S FJ PP GG G RP

15 HPLC-UV (280 nm) Ác. Clorogénico Catequina Procianidina B1 Quercetina-3-glucósido Procianidina B2 Epicatequina Canferol-3-glucósido + Quercetina-3 ramnósido Floridzina RP GG Fj S G PP MS MF BE

16 Ácido clorogénico Epicatequina Catequina Procianidina (B1+B2) mg / 100g maçã Floridzina Quercetina-3-glucósido Canferol-3-glucósido + Quercetina-3-ramnósido MF RP BE S PP MS GG FJ G 164,7 159,5 144,6 105,0 88,5 86,0 80,3 80,3 68,4 mg EAG/100g POLIFENÓIS TOTAIS

17 grape residues Clean technologies Bioactive Extract (containing Resveratrol,Quercetin and Kampferol ) High antioxidant activity Inhibits LDL oxidation Anti-proliferative effect on human cancer cell lines antiviral activity against Ad-5 adenovirus (preliminary study) anti-inflammatory activity

18 Encontro Ciência um TEAC Antioxidant activity NGE Q KP RV Q/KP/RV Q/KP Q/RV KP/RV Abs (234 nm) Controlo LDL oxidation NGE (21,2mg/L) 0.7 NGE (28,3mg/L) 0.6 NGE (42,5mg/L) 0.5 Q+RV+KP t (min) HT29 viability (%of control) Antiproliferative effect on HT Quercetin concentration (mg/l) Quercetine F o ld P r o d u c t io n IL extract 0.0 N G E Q u e r Anti-inflammatory activity K P R V T Q u e r /K P /R V T Q u e r /K P Q u e r /R V T K P /R V T C ( T N F ) C Synergistic effects among different phytochemicals present in the natural extract

19 More efficient therapeutics Better quality of life New and improved controlled delivery sytems

20 ScF Technology Particle Engineering and Controlled Delivery Growing interest in improved delivery systems Drawbacks of traditional particle formation methods (crushing/milling, crystallisation/precipitation) Regulatory demand for reduced residual solvent levels in the final products SCF processing very attractive: - Clean technology - Possibility of processing thermolabile molecules - High purity of products

21 Supercritical Fluids

22 Supercritical Fluids. Densities. Solvating powers <> liquids. Diffusity. Viscosity <> gases Tc(CO 2 ) = 31.1ºC pc(co 2 ) = 73.8 bar scco 2 ellected fluid

23 ScF Technology Particle Engineering and Controlled Delivery Drug Delivery Applications of Supercritical Fluid Technology Volume 60, Issue 3, Pages (14 February 2008) Impact factor of this journal 2006: 7.977

24 ScF Technology in Particle Engineering and Controlled Delivery Systems Advantages: termo-sensitive or very reactive compounds can be processed non-oxidising atmosphere controlled morphology and size of the particles produced homogeneous drug distribution in the impregnated products solvent can be recycled and reused final product free of solvents single step operation

25 Solid material processing with ScF Particle design technologies Impregnation by adsorption Applications Enhancement of dissolution rate of poorly-soluble active ingredients Nano or micronization of particles Preparation of composite particles Stabilization and delivery of the bioactive ingredients Bio-availability enhancement of drugs Design and preparation of controlledrelease systems

26 Polymers successfully processed using SAS technology: PLA (poly-lactic lactic acid) PLA / PEG (poly-lactic lactic acid/poly ethyleneglicol) PLGA (poly-lactic lactic-co co-glicolic acid) PLGA / PEG Eudragit PCL (Poly-caprolactone) Ethylcellulose / methylcellulose PHB(poly-hydrobutirate)

27 Ethylcellulose PLA-PEG PEG DCM 2 µm 2 µm p = 80bar Eudragit T = 35ºC DCM/DMSO p = 130bar T = 30ºC 2 µm acetone p = 85bar T = 35ºC

28 Lipids Polyglycoside Glycerides Precirol ato 5 Compritol 888 ato Gelucire 50/13 Gelucire 43/01 Lumulse GMS K OH HO O CH 3 O O O CH 3 HO O CH 3 O

29 Naproxen-loaded ethyl/methyl cellulose particles Co-precipitation of acetazolamide and Eudragit Co-precipitation of chalcone with polyglycoside glicerides Caffein in gliceryl-monosterarate Antioxidants in lipid-based particles Aroma encapsulation in lipid-based paricles

30 Preparation of ophthalmic drug delivery systems Drugs: Flurbiprofen Timolol maleate Carriers: T = 35 ºC, 40ºC 100 bar < p < 200 bar T = 40ºC 80 bar < p < 100 bar Development of Therapeutic Contact Lenses Using Supercritical Carbon Dioxide Focus Dailies (Ciba Vision) hydrogel contact lenses P(MMA-EHA-EGDMA) PT Patent PT EP Patent EP US Patent US CA Patent CA Optical properties not affected

31 Ana Matias Ana Nunes Ana Rita Duarte Ana Raquel Sousa Ana Teresa Serra Mariana Costa Raquel Frade and... all my under-graduated students

32 Biology Pharmaceutics Organic Chemistry Nutrigenomics Biochemistry Botanics Analytical Chemistry R&D Inorganic Chemistry Biotechnology Nutrition Medicine

33 National: Animal Cell Technology, ITQB / IBET, UNL (Paula Alves) Pharmacokinetics and Biopharmaceutical Laboratory, ITQB/IBET, UNL (Ana Luísa Simplício) Analytical Chemistry Laboratory, IBET/ITQB, UNL(M. Rosário Bronze) REQUIMTE/CQFB, Departamento de Química Faculdade de Ciências e Tecnologia, UNL (Manuel Nunes da Ponte, Ana Isabel Ricardo, Teresa Casimiro, Rui Duarte, Margarida Cardoso, João Paulo Crespo) Dep. de Engª Química, Univ. Coimbra (Hermínio Sousa, M.Helena Gil) Ciência e Tecnologia de Alimentos, Departamento de Agro Industria e Agronomia Tropical, Instituto Superior de Agronomia, UTL (Luísa Beirão da Costa) Instituto Superior de Ciências da Saúde Egas Moniz (Agostinho Carvalho) Instituto Gulbenkian Ciência (Carlos Penha Gonçalves) Encontro Ciência Collaborations Faculdade de Farmácia De Lisboa (M.R.Bronze, M. Eduardo Figueira) International: Dep. of Chemical Engineering and Chemical Technology, Imperial College, London (Sergei Kazarian) Dep. of Chemical Engineering, University of Valladolid, Spain (M.José Coccero) Laboratoire de Génie Procédés des Solides Divisés, École des Mines d Albi-Carmaux, France (Jacques Fages) Laboratory of Applied Thermodynamics and Phase Equilibria, Delft University of Technology, Faculty of Applied Sciences, Netherlands (Cor Peters) Laboratoire d'ingénierie des Matériaux et des Hautes Pressions Université Paris 13, Institut Galilée, Paris (Pascale Subra)