English By:Freag, MS (Freag, May S.)[ 1 ] ; Saleh, WM (Saleh, Wedad M.)[ 2 ] ; Abdallah, OY (Abdallah, Ossama Y.)[ 1 ]
CARBOHYDRATE POLYMERS
Volume: 188
Pages: 108-120
DOI: 10.1016/j.carbpol.2018.01.095
Published: MAY 15 2018
Document Type:Article
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In the current study, laminated chitosan (CS): hydroxypropyl methylcellulose (HPMC) composite sponges were exploited as solid matrices for buccal delivery of tripterine phytosomes functionalized with novel mucopenetrating protamine layer (PRT-TRI-PHY). Tripterine (TRI) is a herbal drug widely investigated as a potential anticancer candidate against various types of cancers. However, clinical use of TRI is handicapped by its low oral bioavailability. To surmount TRI pharmaceutical obstacles, TRI phytosomes (TRI-PHY) were prepared using solvent evaporation technique then coated with a protamine layer via electrostatic assembly process. The developed PRT-TRI-PHY showed a nano-metric size of 250 nm and positive zeta potential (+21.6 mV). Sponges loaded with PRT-TRI-PHY demonstrated a sustained release profile with superior mucoadhesion characteristics compared with the counterparts loaded with uncoated TRI-PHY. The ex-vivo permeation study via chicken pouch mucosa revealed that sponges loaded with PRT-TRI-PHY demonstrated 2.3-folds higher flux value compared with sponges loaded with uncoated TRI-PHY. Additionally, in-vivo pharmacokinetic study in healthy rabbits revealed the significantly higher bioavailability of PRT-TRI-PHY compared with TRI-PHY with relative bioavailability of 244%. Conclusively, mucoadhesive CS-HPMC sponges loaded with a novel mucopenetrating nanocarrier, PRT-TRI-PHY, could significantly improve the absorption of tripterine via buccal mucosa which would be of prime importance for its clinical utility.
Author Keywords:Buccal delivery; Chitosan; Composite sponges; Protamine; Phytosomes; Tripterine
KeyWords Plus:BUCCAL DRUG-DELIVERY; GENE DELIVERY; ORAL BIOAVAILABILITY; LIPID NANOPARTICLES; FORMULATION; CELASTROL; CELLS; PLATFORMS; CARRIERS; PEPTIDE
Reprint Address: Freag, MS (reprint author)
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Alexandria Univ, Fac Pharm, 1 Azarita Sq, Alexandria, Egypt. |
Addresses:
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[ 1 ] Alexandria Univ, Dept Pharmaceut, Fac Pharm, Alexandria, Egypt |
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[ 2 ] Omar Al Mukhtar Univ, Dept Pharmaceut, Fac Pharm, Al Bayda, Libya |
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ELSEVIER SCI LTD, THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, OXON, ENGLAND
Research Areas:Chemistry; Polymer Science
Web of Science Categories:Chemistry, Applied; Chemistry, Organic; Polymer Science