Nanoparticle Preparation of Pentagamavunon-0 Using Medium Viscous Chitosan Matrix Cross Linked by Sodium Tripolyphosphate Through Ionic Gelation Mechanism as Anti-Inflammatory Candidate

https://doi.org/10.22146/farmaseutik.v13i2.40916

Adhyatmika Adhyatmika(1*), Ronny Martien(2), Hilda Ismail(3)

(1) Departemen Farmasetika Fakultas Farmasi UGM
(2) Jurusan Teknik Kimia Fakultas Teknik UGM
(3) Departemen Kimia Farmasi Fakultas Farmasi UGM
(*) Corresponding Author

Abstract


Pentagamavunon-0 (PGV-0, abbreviated), a curcumin analogue with chemical structure as 2,5-bis(4’-hydroxy-3’-methoxybenzilidin)cyclopentanone, has proven to have anti-inflammatory activity and non-ulcerogenic. However, orally PGV-0 has low bioavailability because of its low solubility. One of the strategy to improve PGV-0 solubility in order to increase bioavailability is using nanoparticle carrier. The aim of the study is to formulate chitosan-PGV-0 nanoparticles through ionic gelation mechanism cross-linked by tripolyphosphate. PGV-0 nanoparticle produced was then characterized for its particle size, morphology, zeta potential, entrapment efficiency, and stability against artificial gastric and intestinal fluids (AGF and AIF). PGV-0 nanoparticle was tested for its anti-inflammatory activity by carrageenan induced inflammatory method, and its enzymatic affinity against enzyme cyclooxygenase (COX)-1 and COX-2. Chitosan-PGV-0 nanoparticles were formulated in the combination of 0,05% PGV-0, 0,05% medium-viscous chitosan and 0,002% TPP. The nanoparticles were 144,37 + 17,41 nm amorphous particles. Amount of PGV-0 entrapped was 99,40 + 0,08 % with +3,8 + 0,27 mV in zeta potential. Stability study in AGF and AIF was shown that 99,64-99,74 % (AGF) and 99,54-99,69 % (AIF) of PGV-0 remains in nanoparticles. Chitosan-PGV-0 nanoparticles at 5 mg/kg body weight was obtain 35,47 % anti-inflammatory activity and has found to have self-affinity against COX enzyme, relatively selective to COX-2.

Keywords


nanoparticle, PGV-0, medium viscous chitosan, tripolyphosphate, anti-inflammation

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References

Asosiasi Rheumatologi Australia, 2008, Patient information on NSAIDs, Arthritis Australia. Amalia E., 2001, Profil kadar senyawa 2,5-bis-(4’-hidroksi-3’-metoksi benzilidin) siklopentanon dalam darah setelah pemberian secara oral pada tikus jantan SD, Skripsi, Fakultas Farmasi UGM, Yogyakarta. Bhardwaj V. dan Kumar MNVR., 2006, Polymeric nanoparticles for oral durg delivery on Nanoparticle technology for drug delivery: Drug and the pharmaceutical science, chapter IX, Taylor dan Francis Group, New York, pp. 231-262. Bisht S., Feldmann, G., Soni, S., Ravi, R., Karikar, C., Maitra, A., dan Maitra, A., 2007, Polymeric Nanoparticle-Encapsulated Curcumin ("nanocurcumin"): a Novel Strategy for Human Cancer Therapy, J. Biomater. Sci. Polymer Edn, 18(2): 205–221. Bowman K., Leong KW., 2006, Chitosan nanoparticles for oral drug and gene delivery, a Review, Int. J. Nanomedicine, 1(2): 117-128. Chabib L., Banne Y., Martien R., Ismail H., 2011, Formulasi nanokurkumin dan uji cellular uptake pada sel kanker, laporan penelitian, Proyek I-MHERE Fakultas Biologi UGM. Chavalittumrong P., Chivapat S., Rattanajarasroj S., Punyamong S., Chuthaputti A., Phisalaphong C., 2002, Chronics toxicity study of curcuminoids in rats, Songklanakarin J. Sci. Technol., 24(4): 633-647. Couvreur, P., Barrat, G., Fattal, E., Legrand, P., Vauthier, C., 2002, Nanocapsule Technology: a Review, Crit. Rev. Ther. Drug Carrier Syst, 19: 99-134. David, Arkeman H., 2008, Evaluation of the oral toxicity of formaldehyde in rats, Universa Medicina, 27(3): 106-112. Fernandez-Urussumo R., Calvo P., Remunant-Lopez C., et al., 1999, Enhancement of nasal absorption of insulin using chitosan nanoparticles, Pharm. Res., 16: 1576-1581. Hakim AR., Nugroho AE., Hakim L., 2006, Profil farmakokinetika Pentagamavunon -0 setelah pemberian kalium pentagamavunonat -0 secara oral pada tikus, Indon. J. Pharm., 17(4): 204-211. Jurenka J S., 2009, Anti-inflammatory properties of curcumin, a major constituent of Curcuma longa: A review of preclinical and clinical research, Alt. Med. Rev., 14(2): 141-153/ Kafshgari MH., Khorram M., Khodadoost M., Khavari S., 2011, Reinforcement of chitosan nanoparticles obtained by an ionic cross-linking process, Iran. Polymer J., 20(5): 445-456. Katzung BG., 1986, Farmakologi Dasar dan Klinik, edisi 3, diterjemahkan oleh Binawati HK., Penerbit Buku Kedokteran EGC, Jakarta. Kustaniah, 2001, Profil kadar senyawa 2,5-bis- (4’ - hidroksi - 3’- metoksi benzilidin) siklopentanon dalam darah setelah pemberian secara oral pada tikus betina SD, Skripsi, Fakultas Farmasi UGM, Yogyakarta.



DOI: https://doi.org/10.22146/farmaseutik.v13i2.40916

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