Influence of additives on swelling and mucoadhesion properties of glyceryl monooleate liquid crystals
DOI:
https://doi.org/10.1590/s2175-97902022e20803Keywords:
Glyceryl monooleate, Liquid crystals, Drug delivery, Swelling, Mucoadhesion, Buccal drug deliveryAbstract
Liquid crystalline systems of glyceryl monooleate/water are used as drug delivery systems due to their complex structure that controls drug diffusion. Mucoadhesive properties of glyceryl monooleate suggest it can be used for buccal delivery. Using additives is a strategy to modify physical and chemical properties of liquid crystalline systems and optimize their performance
as a drug delivery system. However, the presence of additives can significantly alter properties such as phase behavior, swelling and mucoadhesion. Our aim is to investigate the influence of additives on swelling and mucoadhesion of glyceryl monooleate-based liquid crystals, intending them to be used as buccal drug delivery systems. The systems were characterized regarding their mesophases, swelling rate, and mucoadhesion. All the systems studied were able to absorb water and presented mucoadhesion, which is interesting for the development of buccal drug delivery systems. Additives induced phase transitions and affected the swelling performance, while mucoadhesive properties were poorly affected. Propylene glycol increased water uptake, while oleic acid induced the phase transition to the hexagonal phase and reduced the swelling rate. The association of oleic acid (5%) and propylene glycol (10%) resulted in a cubic phase system with strong mucoadhesive properties that can be a potential drug carrier for buccal delivery.
Downloads
References
Alfons K, Engström S. Drug compatibility with the sponge
phases formed in monoolein, water, and propylene glycol or
poly(ethylene glycol). J Pharm Sci. 1998;87(12):1527–30.
Bender J, Ericson MB, Merclin N, Iani V, Rosén A, Engström
S, et al. Lipid cubic phases for improved topical drug
delivery in photodynamic therapy. J Controlled Release.
;106(3):350–60.
Bender J, Jarvoll P, Nydén M, Engström S. Structure
and dynamics of a sponge phase in the methyl deltaaminolevulinate/monoolein/water/propylene glycol system.
J Colloid Interface Sci. 2008;317(2):577–84.
Bisset NB, Boyd BJ, Dong Y. Tailoring liquid crystalline
lipid nanomaterials for controlled release of macromolecules.
Int J Pharm. 2015;495(1):241–8.
Boyd BJ, Whittaker DV, Khoo S-M, Davey G. Lyotropic
liquid crystalline phases formed from glycerate surfactants
as sustained release drug delivery systems. Int J Pharm.
;309(1-2):218–26.
Brasnett C, Longstaff G, Compton L, Seddon A. Effects
of cations on the behaviour of lipid cubic phases. Sci Rep.
;7:8229.
Carvalho FC, Bruschi ML, Evangelista RC, Gremião MPD.
Mucoadhesive drug delivery systems. Brazilian J Pharm Sci.
;46(1):1–17.
Chang C-M, Bodmeier R. Effect of dissolution media and
additives on the drug release from cubic phase delivery
systems. J Controlled Release. 1997;46(3):215–22.
Dante M de CL, Borgheti-Cardoso LN, Fantini MC de
A, Praça FSG, Medina WSG, Pierre MBR, et al. Liquid
crystalline systems based on glyceryl monooleate and
penetration enhancers for skin delivery of celecoxib:
characterization, in vitro drug release, and in vivo studies. J
Pharm Sci. 2018;107(3):870–8.
Dash AK, Gong Z, Miller DW, Huai-Yan H, Laforet JP.
Development of a rectal nicotine delivery system for the
treatment of ulcerative colitis. Int J Pharm. 1999;190(1):21–
Esposito E, Carducci F, Mariani P, Huang N, Simelière F,
Cortesi R, et al. Monoolein liquid crystalline phases for
topical delivery of crocetin. Colloids Surf B. 2018;171:67–74.
Esposito E, Carotta V, Scabbia A, Trombelli L, D’Antona
P, Menegatti E, et al. Comparative analysis of tetracyclinecontaining dental gels: Poloxamer- and monoglyceride-based
formulations. Int J Pharm. 1996;142(1):9–23.
Guo C, Wang J, Cao F, Lee RJ, Zhai G. Lyotropic liquid
crystal systems in drug delivery. Drug Discov Today.
;15(23-24):1032–40.
Kumar M. K, Shah MH, Ketkar A, Mahadik KR, Paradkar A.
Effect of drug solubility and different excipients on floating
behaviour and release from glyceryl monooleate matrices.
Int J Pharm 2004;272(1-2):151–60.
Lara MG, Bentley MVLB, Collett JH. In vitro drug release
mechanism and drug loading studies of cubic phase gels. Int
J Pharm. 2005;293(1-2):241–50.
Lee J, Choi SU, Yoon MK, Choi YW. Kinetic characterization
of swelling of liquid crystalline phases of glyceryl
monooleate. Arch Pharm Res. 2003;26:880–5.
Lee J, Kellaway IW. Combined effect of oleic acid and
polyethylene glycol 200 on buccal permeation of [D-Ala2,
D-Leu5]enkephalin from a cubic phase of glyceryl
monooleate. Int J Pharm. 2000;204(1-2):137–44.
Lee J, Young SA, Kellaway IW. Water quantitatively induces
the mucoadhesion of liquid crystalline phases of glyceryl
monooleate. J Pharm Pharmacol. 2001;53(5):629–36.
Li Q, Cao J, Li Z, Chu X. Cubic Liquid Crystalline Gels
Based on Glycerol Monooleate for Intra-articular Injection.
AAPS Pharm Sci Tech. 2018;19(2):858–65.
Libster D, Aserin A, Garti N. Interactions of
biomacromolecules with reverse hexagonal liquid crystals:
Drug delivery and crystallization applications. J Colloid
Interface Sci. 2011;356(2):375–86.
Lopes LB, Lopes JLC, Oliveira DCR, Thomazini JA, Garcia
MTJ, Fantini MC de A, et al. Liquid crystalline phases of
monoolein and water for topical delivery of cyclosporin A:
Characterization and study of in vitro and in vivo delivery.
Eur J Pharm Biopharm. 2006;63(2):146–55.
Madheswaran T, Baskaran R, Thapa RK, Rhyu JY, Choi HY,
Kim JO, et al. Design and in vitro evaluation of finasteride-loaded liquid crystalline nanoparticles for topical delivery.
AAPS Pharm Sci Tech. 2013;14(1):45–52.
Merclin N, Bender J, Sparr E, Guy RH, Ehrsson H,
Engström S. Transdermal delivery from a lipid sponge
phase--iontophoretic and passive transport in vitro of
-aminolevulinic acid and its methyl ester. J Controlled
Release. 2004;100(2):191–8.
Milak S, Zimmer A. Glycerol monooleate liquid crystalline
phases used in drug delivery systems. Int J Pharm.
;478(2):569–87.
Nakamoto, RY. Use of a saliva substitute in postradiation
xerostomia. J of Prost Dent. 1979;42(5):539-542.
Nielsen LS, Schubert L, Hansen J. Bioadhesive drug delivery
systems. I. Characterisation of mucoadhesive properties
of systems based on glyceryl mono-oleate and glyceryl
monolinoleate. Eur J Pharm Sci. 1998;6(3):231–9.
Norling T, Lading P, Engström S, Larsson K, Krog N,
Nissen SS. Formulation of a drug delivery system based
on a mixture of monoglycerides and triglycerides for use
in the treatment of periodontal disease. J Clin Periodontol.
;19(9 Pt2):687–92.
Nunes KM, Teixeira CCC, Kaminski RCK, Sarmento VHV,
Couto RO, Pulcinelli SH, et al. The monoglyceride content
affects the self-assembly behavior, rheological properties,
syringeability, and mucoadhesion of in situ–gelling liquid
crystalline phase. J Pharm Sci. 2016;105(8):2355–64.
Okonogi S, Khongkhunthain S, Bunyaratavej P, Thusaphorn
T, Umpriwan R. Development of local injectable dental
gel: the influence of certain additives on physicochemical
properties of glycerylmonooleate-based formulations. Drug
Dev Ind Pharm. 2004;30(4):347–57.
Peng X, Wen X, Pan X, Wang R, Chen B, Wu C. Design and in
vitro evaluation of capsaicin transdermal controlled release
cubic phase gels. AAPS PharmSciTech. 2010;11(3):1405–10.
Phan S, Fong WK, Kirby N, Hanley T, Boyd BJ. Evaluating
the link between self-assembled mesophase structure and
drug release. Int J Pharm. 2011;421(1):176–82.
Rajabalaya R, Musa MN, Kifli N, David SR. Oral and
transdermal drug delivery systems: Role of lipid-based
lyotropic liquid crystals. Drug Des Devel Ther. 2017;11:393–
Rizwan SB, Hanley T, Boyd BJ, Rades T, Hook S. Liquid
crystalline systems of phytantriol and glyceryl monooleate
containing a hydrophilic protein: Characterisation, swelling
and release kinetics. J Pharm Sci. 2009;98(11):4191–204.
Sallam AS, Khalil E, Ibrahim H, Freij I. Formulation of
an oral dosage form utilizing the properties of cubic liquid
crystalline phases of glyceryl monooleate. Eur J Pharm
Biopharm. 2002;53(3):343–52.
Schott H. Kinetics of swelling of polymers and their gels. J
Pharm Sci. 1992;81(5):467–70.
Shah MH, Paradkar A. Effect of HLB of additives on the
properties and drug release from the glyceryl monooleate
matrices. Eur J Pharm Biopharm. 2007;67(1):166–74.
Shah JC, Sadhale Y, Chilukuri DM. Cubic phase gels as drug
delivery systems. Adv Drug Deliv Rev. 2001;47(2-3):229–50.
Smart JD. The basics and underlying mechanisms of
mucoadhesion. Adv Drug Deliv Ver. 2005;57(11):1556–68.
Souza C, Watanabe E, Borgheti-Cardoso LN, Fantini MC de
A, Lara MG. Mucoadhesive system formed by liquid crystals
for buccal administration of poly(hexamethylene biguanide)
hydrochloride. J Pharm Sci 2014;103(12):3914–23.
Wang X, Zhang Y, Gui S, Huang J, Cao J, Li Z, et al.
Characterization of lipid-based lyotropic liquid crystal and
effects of guest molecules on its microstructure: a systematic
review. AAPS Pharm Sci Tech. 2018;19(5):2023–40.
Zabara A, Mezzenga R. Controlling molecular transport
and sustained drug release in lipid-based liquid crystalline
mesophases. J Controlled Release. 2014;188:31–43.
Downloads
Published
Issue
Section
License
Copyright (c) 2022 Brazilian Journal of Pharmaceutical Sciences
This work is licensed under a Creative Commons Attribution 4.0 International License.
All content of the journal, except where identified, is licensed under a Creative Commons attribution-type BY.
The on-line journal has open and free access.
