Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2018 Feb 11;10(2):175.
doi: 10.3390/polym10020175.

Formulation of Carbopol®/Poly(2-ethyl-2-oxazoline)s Mucoadhesive Tablets for Buccal Delivery of Hydrocortisone

Affiliations

Formulation of Carbopol®/Poly(2-ethyl-2-oxazoline)s Mucoadhesive Tablets for Buccal Delivery of Hydrocortisone

Leire Ruiz-Rubio et al. Polymers (Basel). .

Abstract

Poly(2-ethyl-2-oxazoline) has become an excellent alternative to the use of poly(ethylene glycol) in pharmaceutical formulations due to its valuable physicochemical and biological properties. This work presents a formulation of poorly-water soluble drug, hydrocortisone, using interpolymer complexes and physical blends of poly(2-ethyl-2-oxazoline)s and two Carbopols® (Carbopol 974 and Carbopol 971) for oromucosal administration. The swelling, hydrocortisone release and mucoadhesive properties of a series of tablet formulations obtained by combination of different Carbopols with poly(2-ethyl-2-oxazoline)s of different molecular weights have been evaluated in vitro.

Keywords: Carbopol®; interpolymer complexes; mucoadhesion; poly(2-ethyl-2-oxazoline).

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Yields of interpolymer complexes (wt %) for different Carbopol/poly(2-ethyl-2-oxazoline) systems in water and at pH 2.
Figure 2
Figure 2
Analysis of Carbopol 974/poly(2-ethyl-2-oxazoline) 500 complex, and pure components by: (a) FTIR; and (b) DSC.
Figure 3
Figure 3
The total work of adhesion (left) and detachment force (right) on porcine buccal tissues at 37 °C for: (a) Carbopol 974/poly(2-ethyl-2-oxazoline) tablets; and (b) Carbopol 971/poly(2-ethyl-oxazoline) tablets.
Figure 4
Figure 4
Swelling degree of pure polymers in simulated saliva.
Figure 5
Figure 5
Swelling degree and photographs of the tablets of Carbopols/Poly(2-ethyl-2-oxazoline)s in saliva at 37 °C at regular time intervals: (a) physical mixture; (b) interpolymer complexes formed in water; and (c) interpolymer complexes formed at pH 2 (A Carbopol 974; and B. Carbopol 971).
Figure 6
Figure 6
Release profiles of hydrocortisone from the tablets composed of poly(2-ethyl-2-oxazoline)s/Carbopols in simulated saliva at 37 °C: (a) physical mixture; (b) interpolymer complexes formed in water; and (c) interpolymer complexes formed at pH 2. (A Carbopol 974; and B. Carbopol 971).

References

    1. Stegemann S., Leveiller F., Franchi D., de Jong H., Lindén H. When poor solubility becomes an issue: From early stage to proof of concept. Eur. J. Pharm. Sci. 2007;31:249–261. doi: 10.1016/j.ejps.2007.05.110. - DOI - PubMed
    1. Khadka P., Ro J., Kim H., Kim I., Kim J.T., Kim H., Cho J.M., Yun G., Lee J. Pharmaceutical particle technologies: An approach to improve drug solubility, dissolution and bioavailability. Asian J. Pharm. Sci. 2014;9:304–316. doi: 10.1016/j.ajps.2014.05.005. - DOI
    1. Kalepu S., Nekkanti V. Insoluble drug delivery strategies: Review of recent advances and business prospects. Acta Pharm. Sin. B. 2015;5:442–453. doi: 10.1016/j.apsb.2015.07.003. - DOI - PMC - PubMed
    1. Schulze J.D.R., Waddington W.A., Ell P.J., Parsons G.E., Coffin M.D., Basit A.W. Concentration-Dependent Effects of Polyethylene Glycol 400 on Gastrointestinal Transit and Drug Absorption. Pharm. Res. 2003;20:1984–1988. doi: 10.1023/B:PHAM.0000008046.64409.bd. - DOI - PubMed
    1. Harris J.M., Dust J.M., McGill R.A., Harris P.A., Edgell M.J., Sedaghat-Herati R.M., Karr L.J., Donnelly D.L. Water-Soluble Polymers. Volume 467. American Chemical Society; Washington, DC, USA: 1991. New Polyethylene Glycols for Biomedical Applications; pp. 27–418. (ACS Symposium Series).

LinkOut - more resources