International Journal of Pharmaceutical Investigation, 2013, 3, 4, 194-202.
DOI: 10.4103/2230-973X.121292
Published: November 2013
Type: Original Article
Authors:
Neha S Raut
Department of Pharmaceutics, Smt. Kishoritai Bhoyar College of Pharmacy, New Kamptee, Nagpur, Maharashtra, India.
Prasad R Deshmukh
Department of Pharmaceutics, Smt. Kishoritai Bhoyar College of Pharmacy, New Kamptee, Nagpur, Maharashtra, India.
Milind J Umekar
Department of Pharmaceutics, Smt. Kishoritai Bhoyar College of Pharmacy, New Kamptee, Nagpur, Maharashtra, India.
Nandkishor R Kotagale
Department of Pharmaceutics, Smt. Kishoritai Bhoyar College of Pharmacy, New Kamptee, Nagpur, Maharashtra, India.
ABSTRACT
Introduction: Alginates can be tailored chemically to improve solubility, physicochemical and biological properties and its complexation with metal ion is useful for controlling the drug release. Materials And Methods: Synthesized N,O-dimethyl, N-methyl, or N-Benzyl hydroxylamine derivatives of sodium alginate were subsequently complexed with zinc to form beads. Hydroxamation of sodium alginate was confirmed by Fourier transform infra-red spectroscopy (FTIR) and differential scanning calorimetry (DSC). Results: The synthesized polymeric material exhibited reduced aqueous, HCl and NaOH solubility. The hydroxamated derivatives demonstrated pulsed release where change in pH of the dissolution medium stimulated the atenolol release. Conclusion: Atenolol loaded Zn cross-linked polymeric beads demonstrated the sustained the plasma drug levels with increased half-life. Although the synthesized derivatives greatly altered the aqueous solubility of sodium alginate, no significant differences in in vitro and in vivo atenolol release behavior amongst the N,O-dimethyl, N-methyl, or N-Benzyl hydroxylamine derivatives of sodium alginate were observed.
Keywords: Atenolol, Hydroxylamine .derivatives, Metal-polymer cross-linked beads, Pulsatile release, Sodium alginate.