Effervescent proliposomes for aerosol delivery to paranasal sinuses

Korale, Aluthweediya K.O.D. (2016) Effervescent proliposomes for aerosol delivery to paranasal sinuses. Doctoral thesis, University of Central Lancashire.

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This study aims to design and develop effervescent proliposomes that could disintegrate in water and liberate liposomes, and to investigate the potential suitability of liposomes generated for aerosolization to target paranasal sinuses. Novel effervescent proliposomes prepared with Soya phosphatidylcholine (SPC) and Dipalmitoylphosphatidylcholine (DPPC) successfully generated stable liposomes with an improved disintegration time of less than 5 min. Differences in lipid composition were found to influence liposome size and drug entrapment of the hydrophobic drug Beclometasone dipropionate (BDP). Mannitol-based formulations developed with DPPC:Chol (1:1) produced liposomes of 7.54±0.15 µm with a drug entrapment efficiency of 82.15±8.29%. Addition of the mucoadhesives alginic acid or chitosan to effervescent proliposomes made with SPC was found to hamper BDP entrapment in liposomes. Effervescent proliposomes produced SPC:Chol liposomes that also proved beneficial for entrapment of the hydrophilic drug Xylometazoline hydrochloride (XH). The Pari Sinus (pulsating aerosol technology) and Pari Sprint (non-pulsating technology) nebulizers were used for liposome delivery to a nasal cast. Choice of carrier did not affect the liposome’s ability to withstand shearing. A novel system of a Sar-Gel® (water indicating paste) coated clear nasal cast fixed to a two-stage impinger system was set up to analyze drug deposition within the nasal cast cavity. Sinus drug deposition with effervescent mannitol, DPPC:Chol formulation was observed to be highest at 48.45±2.75 cm2 with pulsation compared to deposition of 35.52±11.11 cm2 without pulsation. Drug distribution studies indicated that the Pari Sinus deposited 10.47±2.9% drug, while the Pari Sprint deposited only 4.6±1.4%. The degree of drug loss was higher with conventional liposomes in the Pari Sinus nebulizer, indicating that the degree of bilayers disruption depended on formulation.

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