Rutin yüklü PLGA Nanopartiküller; Farklı Yöntemler Kullanılarak Sentezi ve Karakterizasyonu

Year 2019, Volume: 9 Issue: 2, 922 - 932, 01.06.2019

Tuğçe Kirik Kadriye Kızılbey

https://doi.org/10.21597/jist.481180

Cited By: 2

Abstract

Bazı bitkiler ile özellikle turunçgiller gibi meyvelerde ve kabuklarında bulunan bir flavonol glikozit olan Rutin molekülünün zayıf çözünürlüğü nedeniyle canlı sistemde biyoyararlanımı oldukça düşüktür. Bu çalışmada, Rutin molekülünün biyoyararlanımı arttırmak için tekli emülsiyon solvent buharlaştırma (o/w), nano çöktürme ve tuz etkisi ile çöktürme gibi farklı yöntemler kullanılarak Rutin yüklü PLGA nanopartikülleri sentezlenmiştir. Bu nanopartiküller % enkapsülasyon etkinliği, ortalama parçacık boyutu, çoklu dağılım indisi, Zeta potansiyel, Fourier dönüşümlü kızılötesi spektroskopisi ve taramalı elektron mikroskobu analizleri ile karakterize edilmiştir. NP3 ve NP5’in in vitro ortamda Rutin salımı incelenmiştir. NP5’den % Rutin salımı 48 saatte %41 oranına ulaşmıştır. Yapılan bu çalışmada sentezlenen Rutin-yüklü nanopartiküllerin, ileride nanotıp alanında gelişmiş ve çok yönlü çalışmalar için uygun bir aday olması hedeflenmektedir.

Keywords

Rutin, PLGA, Emülsiyon, Nanoçöktürme, Biyoyararlanım

Thanks

Yıldız Teknik Üniversitesi Biyomühendislik Bölümü Öğretim Üyesi Yrd. Doç. Dr. Zeynep MUSTAFAEVA AKDESTE ve Doç. Dr. Serap DERMAN’a deneysel çalışmalarım boyunca sağlamış oldukları laboratuvar olanaklarından dolayı teşekkürlerimi sunarım.

Rutin Loaded PLGA Nanoparticles; Synthesis by using Different Methods and Characterization

Abstract

Due to the poor solubility of the Rutin molecule, which is a flavonol glycoside found in some plants and especially in citrus fruits and shells, its bioavailability is quite low. In this study, Rutin-loaded-PLGA nanoparticles were synthesized by using different methods such as single emulsion solvent evaporation, nanoprecipitation and salting out, in order to increase the bioavailability of Rutin. These nanoparticles were characterized by their encapsulation efficiency %, average particle size, polydispersity index, Zeta potential, Fourier transform infrared spectroscopy and scanning electron microscopy analysis. In vitro Rutin release studies of NP3 and NP5 were investigated. Rutin release from NP5 reached 41% in 48 hours. It is aimed that the Rutin-loaded nanoparticles synthesized in this work will be suitable candidates for future multidisciplinary studies developed in nanomedicine.

Keywords

Rutin, PLGA, Emulsion, Nanoprecipitation, Bioavailability

References

• Al-Dhabi N A, Arasu M V, Park C H and Park S U, 2015. An up-to-date review of rutin and its biological and pharmacological activities. Experimental and Clinical Science, 14: 59-63.
• Bilia A R, Isacchi B, Righeschi C, Guccione C and Bergonzi M C, 2014. Flavonoids loaded in nanocarriers: an opportunity to increase oral bioavailability and bioefficacy. Food and Nutrition Sciences, 5(13): 1212-1327.
• Budhian A S, Siegel S J and Winey K I, 2007. Haloperidol-loaded PLGA nanoparticles: systematic study of particle size and drug content. International Journal of Pharmaceutics, 336(2): 367-375.
• Calabro M, Tommasini S, Donato P, Stancanelli R, Raneri D, Catania S, Costa C, Villari V, Ficarra P and Ficarra R, 2005. The rutin/β-cyclodextrin interactions in fully aqueous solution: spectroscopic studies and biological assays. Journal of Pharmaceutical and Biomedical Analysis, 36(5): 1019-1027.
• Cherbi R, Saidi M, Yousfi M and Rahmani Z, 2016. Total phenols, total flavonoids contents and free radical scavenging activity of seeds extracts of Lawsonia alba (henna) from Algeria. Der Pharma Chemica, 8(11):216-221.
• Chua L S, 2013. A review on plant-based rutin extraction methods and its pharmacological activities. Journal of Ethnopharmacology, 150(3): 805-817.
• Das S, Das J, Samadder A, Paul A and Khuda-Bukhsh A R, 2013. Strategic formulation of apigenin-loaded PLGA nanoparticles for intracellular trafficking, DNA targeting and improved therapeutic effects in skin melanoma in vitro. Toxicology letters, 223(2): 124-138.
• de Oliveira I R, Fernandes W Z and Vieira I C, 2006. Development of a biosensor based on gilo peroxidase immobilized on chitosan chemically crosslinked with epichlorohydrin for determination of rutin. Journal of Pharmaceutical and Biomedical Analysis, 41(2): 366-372.
• Derman S, 2015. Caffeic acid phenethyl ester loaded PLGA nanoparticles: effect of various process parameters on reaction yield, encapsulation efficiency, and particle size. Journal of Nanomaterials, 16(1): 318-330.
• Derman S, Kızılbey K and Akdeste Z M, 2013. Polymeric nanoparticles. Sigma Journal of Engineering and Natural Sciences, 31: 107-120.
• Dudhani A R and Kosaraju S L, 2010. Bioadhesive chitosan nanoparticles: Preparation and characterization. Carbohydrate Polymers, 81(2): 243-251.
• Heim K E, Tagliaferro A R and Bobilya D J, 2002. Flavonoid antioxidants: chemistry, metabolism and structure-activity relationships. The Journal of Nutritional Biochemistry, 13(10): 572-584.
• Hooresfand Z, Ghanbarzadeh S and Hamishehkar H, 2015. Preparation and characterization of rutin-loaded nanophytosomes. Pharmaceutical Sciences, 21(3): 145-151.
• Kızılbey K, 2012. Melanoma hastalığını oluşturan sentetik peptidlerin poliakrilikasit ve kopolimerleri ile konjugasyonu, Yıldız Teknik Üniversitesi Fen Bilimleri Enstitüsü, Doktora Tezi (Basılmış).
• Kumar G, Shafiq N and Malhotra S, 2012. Drug-loaded PLGA nanoparticles for oral administration: fundamental issues and challenges ahead. Critical Reviews™ in Therapeutic Drug Carrier Systems, 29(2):149-182.
• Mainardes R M and Evangelista R C, 2005. PLGA nanoparticles containing praziquantel: effect of formulation variables on size distribution. International Journal of Pharmaceutics, 290(1-2): 137-144.
• Makadia H K and Siegel S J, 2011. Poly lactic-co-glycolic acid (PLGA) as biodegradable controlled drug delivery carrier. Polymers, 3(3): 1377-1397.
• Manach C, Morand C, Demigné C, Texier O, Régérat F and Rémésy C, 1997. Bioavailability of rutin and quercetin in rats. FEBS Letters, 409(1): 12-16.
• Patil A G and Jobanputra A H, 2015. Rutin-chitosan nanoparticles: fabrication, characterization and application in dental disorders. Polymer-Plastics Technology and Engineering, 54(2): 202-208.
• Pool H, Quintanar D, de Dios Figueroa J, Mano C M, Bechara J E H, Godínez L A and Mendoza S, 2012. Antioxidant effects of quercetin and catechin encapsulated into PLGA nanoparticles. Journal of Nanomaterials, 86-97.
• Sah E and Sah H, 2015. Recent trends in preparation of poly (lactide-co-glycolide) nanoparticles by mixing polymeric organic solution with antisolvent. Journal of Nanomaterials, 16(1): 61.
• Song X, Zhao Y, Hou S, Xu F, Zhao R, He J, Cai Z, Li Y and Chen Q, 2008. Dual agents loaded PLGA nanoparticles: systematic study of particle size and drug entrapment efficiency. European Journal of Pharmaceutics and Biopharmaceutics, 69(2): 445-453.
• Song X, Zhao Y, Wu W, Bi Y, Cai Z, Chen Q, Li Y and Hou S, 2008. PLGA nanoparticles simultaneously loaded with vincristine sulfate and verapamil hydrochloride: systematic study of particle size and drug entrapment efficiency. International Journal of Pharmaceutics, 350(1-2): 320-329.
• Soppimath K S, Aminabhavi T M, Kulkarni A R and Rudzinski W E, 2001. Biodegradable polymeric nanoparticles as drug delivery devices. Journal of Controlled Release, 70(1-2): 1-20.
• Stuard S, Cesarone M R, Belcaro G, Dugall M, Ledda A, Cacchio M, Ricci A, Ippolito E, Di Renzo A and Grossi M G, 2008. Five-year treatment of chronic venous insufficiency with O-(β-hydroxyethyl)-rutosides: Safety aspects. International Journal of Angiology, 17(03): 143-148.
• Wang H, Zhao Y, Wu Y, Hu Y, Nan K, Nie G and Chen H, 2011. Enhanced anti-tumor efficacy by co-delivery of doxorubicin and paclitaxel with amphiphilic methoxy PEG-PLGA copolymer nanoparticles. Biomaterials, 32(32): 8281-8290.
• Webster R, Gawde M and Bhattacharya R, 1996. Protective effect of rutin, a flavonol glycoside, on the carcinogen-induced DNA damage and repair enzymes in rats. Cancer Letters, 109(1-2): 185-191.
• Yang J, Guo J and Yuan J, 2008. In vitro antioxidant properties of rutin. LWT-Food Science and Technology, 41(6): 1060-1066.
• Zvezdanović J B, Stanojević J S, Marković D Z and Cvetković D J, 2012. Irreversible UV-induced quercetin and rutin degradation in solution, studied by UV-spectrophotometry and HPLC chromatography. Journal of the Serbian Chemical Society, 77(3): 297-312.