Budesonide-Hydroxypropyl-β-Cyclodextrin Inclusion Complex in Poloxamer 407 and Poloxamer 407/403Systems: A Structural Study by Small Angle X-Ray Scattering (SAXS)
Journal Title: Biomedical Journal of Scientific & Technical Research (BJSTR) - Year 2018, Vol 10, Issue 5
Abstract
Poloxamer (PL), copolymers composed of polyethylene oxide (PEO) and polypropylene oxide (PPO) units, have been studied for several applications considering them as tensoatives, stabilizers, solubilizers and nano carriers. For pharmaceutical applications, they are of great interest for the development of drug-delivery systems as unique or binary systems (association of two types of PL) and for forming supramolecular complexes with other molecules (i.e. 2-hydroxypropyl-p-cyclodextrin-HP-β-CD), especially for poorly soluble drugs, such as budesonide (BUD), a glucocorticoid widely used for the treatment of ulcerative colitis. This study reports the structural studies, by Small Angle X-ray Scattering (SAXS), looking forward the understanding of the mechanisms and models of interaction between BUD, HP-β-CD or BUD-HP-β-CD inclusion complex and PL407 or its binary system, PL407-PL403. The SAXS analysis revealed the systems organization in a lamellar structure, for PL407 and PL407-PL403, even after addition of HP-β-CD, BUD or the BUD-HP-β-CD inclusion complex. Those differences are results of typical interactions between BUD or HP-β-CD with the micellar core (PPO region), while the presence of inclusion complex is observed on the micellar hydrated region (PEO). Those results are of great interest on the study of physico-chemical aspects applied to the development of drug-delivery formulations.Systemic glucocorticoids have been traditionally used to induce remission in patients with inflammatory bowel disease such as ulcerative colitis (UC), due to their potent anti-inflammatory effects. However, the wide range of adverse effects associated with these drugs stimulated the development of new agents with safer pharmacological profile and predominant local anti-inflammatory activity, such as budesonide (BUD) [1,2]. Cyclodextrins (CD) have been used as adjuvants in different pharmaceutical formulations due to their ability to form of inclusion complexes. In special, the p-CD derivative, 2-hydroxypropyl-p-cyclodextrin (HP-β-CD), is an effective alternative for complexation with poorly soluble drugs [3,4] such as BUD. For pharmaceutical applications, it has been reported the development of ternary complexes, i.e., comprising three different molecular entities. Two of those compounds refer to the drug and CD, while the third one may have different origins and purposes, such as natural or synthetic polymers [5]. In addition to CD, polymers such as poloxamers (PL) improve physico-chemical properties of the drug, as well as the entrapment and the efficiency of release, also optimizing the cost, toxicity and the production of the scaled-up pharmaceutical formulations [4].
Authors and Affiliations
Margareth KKD Franco, Melissa I Alkschbirs, Alessandra CS Akkarid, Fabiano Yokaichiya, Daniele Ribeiro de Araujo
Keywords
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- EP ID EP592325
- DOI 10.26717/BJSTR.2018.10.002002
- Views 142
- Downloads 0
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