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Lipid cubic systems for sustained and controlled delivery of antihistamine drugs

DOI: 10.1021/acs.molpharmaceut.1c00279 DOI Help

Authors: Michele Dully (University of Limerick) , Miriama Ceresnakova (University of Limerick) , David Murray (COOK Ireland Limited) , Tewfik Soulimane (University of Limerick) , Sarah P. Hudson (University of Limerick)
Co-authored by industrial partner: Yes

Type: Journal Paper
Journal: Molecular Pharmaceutics , VOL 3

State: Published (Approved)
Published: September 2021

Open Access Open Access

Abstract: Antihistamines are capable of blocking mediator responses in allergic reactions including allergic rhinitis and dermatological reactions. By incorporating various H1 receptor antagonists into a lipid cubic phase network, these active ingredients can be delivered locally over an extended period of time owing to the mucoadhesive nature of the system. Local delivery can avoid inducing unwanted side effects, often observed after systematic delivery. Lipid-based antihistamine delivery systems are shown here to exhibit prolonged release capabilities. In vitro drug dissolution studies investigated the extent and release rate of two model first-generation and two model second-generation H1 antagonist antihistamine drugs from two monoacyglycerol-derived lipid models. To optimize the formulation approach, the systems were characterized macroscopically and microscopically by small-angle X-ray scattering and polarized light to ascertain the mesophase accessed upon an incorporation of antihistamines of varying solubilities and size. The impact of encapsulating the antihistamine molecules on the degree of mucoadhesivity of the lipid cubic systems was investigated using multiparametric surface plasmon resonance. With the ultimate goal of developing therapies for the treatment of allergic reactions, the ability of the formulations to inhibit mediator release utilizing RBL-2H3 mast cells with the propensity to release histamine upon induction was explored, demonstrating no interference from the lipid excipient on the effectiveness of the antihistamine molecules.

Journal Keywords: lipid cubic phase; controlled delivery; hydrophobic active pharmaceuticals; antihistamines; mucoadhesion; SAXS

Subject Areas: Biology and Bio-materials, Chemistry, Medicine

Instruments: B21-High Throughput SAXS

Added On: 22/09/2021 14:44


Discipline Tags:

Drug Delivery Non-Communicable Diseases Health & Wellbeing Biochemistry Chemistry Organic Chemistry Life Sciences & Biotech Allergic Diseases

Technical Tags:

Scattering Small Angle X-ray Scattering (SAXS)