title: Synthesis of Polyamidoamine Dendrimer for Encapsulating Tetramethylscutellarein for Potential Bioactivity Enhancement.
abstract: The biomedical potential of flavonoids is normally restricted by their low water solubility. However, little has been reported on their encapsulation into polyamidoamine (PAMAM) dendrimers to improve their biomedical applications. Generation four (G4) PAMAM dendrimer containing ethylenediaminetetraacetic acid core with acrylic acid and ethylenediamine as repeating units was synthesized by divergent approach and used to encapsulate a flavonoid tetramethylscutellarein (TMScu, 1) to study its solubility and in vitro release for potential bioactivity enhancement. The as-synthesized dendrimer and the dendrimer-TMScu complex were characterized by spectroscopic and spectrometric techniques. The encapsulation of 1 into dendrimer was achieved by a co-precipitation method with the encapsulation efficiency of 77.8% ± 0.69% and a loading capacity of 6.2% ± 0.06%. A phase solubility diagram indicated an increased water solubility of 1 as a function of dendrimer concentration at pH 4.0 and 7.2. In vitro release of 1 from its dendrimer complex indicated high percentage release at pH 4.0. The stability study of the TMScu-dendrimer at 0, 27 and 40 °C showed the formulations to be stable when stored in cool and dark conditions compared to those stored in light and warmer temperatures. Overall, PAMAM dendrimer-G4 is capable of encapsulating 1, increasing its solubility and thus could enhance its bioactivity.
authors.affiliation: Chemistry Department, University of Dar es Salaam, College of Natural and Applied Sciences, P.O. Box 35061 Dar es Salaam, Tanzania. dmssjut@gmail.com.|Chemistry Department, St John's University of Tanzania, P.O. Box 47 Dodoma, Tanzania. dmssjut@gmail.com.
authors.forename: Daniel M
authors.initials: DM
authors.lastname: Shadrack
authors.affiliation: Chemistry Department, University of Dar es Salaam, College of Natural and Applied Sciences, P.O. Box 35061 Dar es Salaam, Tanzania. ebmubofu@udsm.ac.tz.
authors.forename: Egid B
authors.initials: EB
authors.lastname: Mubofu
authors.affiliation: Chemistry Department, University of Dar es Salaam, College of Natural and Applied Sciences, P.O. Box 35061 Dar es Salaam, Tanzania. nyandoro@udsm.ac.tz.
authors.forename: Stephen S
authors.initials: SS
authors.lastname: Nyandoro
mesh_terms: D050091:Dendrimers; D004339:Drug Compounding; D065546:Drug Liberation; D004355:Drug Stability; D005029:Ethylenediamines / Q000737:chemistry* / Q000494:pharmacology*; D011073:Polyamines / Q000138:chemical synthesis / Q000737:chemistry*; D066244:Proton Magnetic Resonance Spectroscopy; D012995:Solubility; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
chemical_list: D050091:Dendrimers; D005029:Ethylenediamines; C531249:Poly(amidoamine); D011073:Polyamines; C031234:ethylenediamine
keywords: PAMAM G4 dendrimer; encapsulation; in vitro release; solubilization; stability; tetramethylscutellarein