Abstract

Effective applicability of serum albumin-hyaluronic acid (HyA) conjugates as potential drug delivery colloidal particles having d ∼ 220 – 260 nm average size has been presented for encapsulation of ibuprofen (IBU). Increased IBU content with drug loading of 30 % can be achieved via combination of the serum albumin proteins with biodegradable HyA polysaccharide. After optimization of the synthesis protocols and the characterization of the prepared systems for both bovine (BSA) and human serum albumin (HSA)-based particles, in vitro dissolution and intestinal-specific permeability studies were also performed. It was established that these protein/polysaccharide colloidal carriers have more favourable dissolution, intestinal permeability, and flux features than the unformulated IBU which is greatly controlled by the net charge of serum albumins at pH = 6.50. The nanosized carrier formula, which provides enhanced solubility, accelerated dissolution, and greater permeability, may represent a more controlled, lower dose loading, and gastric mucosa-sparing therapeutic solution in the high-dose IBU therapy.

Highlights

  • The improvement of novel drug delivery systems (DDSs) is of prime interest for the design of novel therapeutic approaches [1]

  • In the first part of this article [15] mIBU/mBSA = 0.25 ratio was used to confirm the applicability of serum albumin/polysaccharide complex carrier on IBU encapsulation by several spectroscopic and thermoanalytical techniques

  • To optimize the maximum amount of IBU to be added to protein, changes in bovine serum albumin (BSA) structure were monitored upon administration of IBU to BSA by CD studies

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Summary

Introduction

The improvement of novel drug delivery systems (DDSs) is of prime interest for the design of novel therapeutic approaches [1]. Due to their biocompatibility and biodegradability the natural polysaccharides are widely applied [2,3,4] in pharmacy; the extreme hydrophilic hyaluronic acid (HyA) is a natural linear glycosaminoglycan affected in different biological processes including cell growth or migration [5]. The role of serum albumins in the development of protein-based delivery systems is well-known [6] owing to the unique ability of binding features [7] as wide range of organic and inorganic compound can bind to the active region of the protein [8].

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