Acyclovir liposomes for intranasal systemic delivery: development and pharmacokinetics evaluation

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• The intranasal route offers an attractive pathway for systemic drug distribution.
• Liposomes serve as biocompatible carriers to enhance drug permeation across the nasal mucosa.
• Developing effective intranasal drug delivery systems is crucial for improving therapeutic outcomes.

Purpose of the Study:

• To formulate acyclovir-loaded liposomes and incorporate them into a poly-N-vinyl-2-pyrrolidone (PVP) mucoadhesive gel.
• To evaluate the entrapment efficiency of acyclovir within different liposomal formulations.
• To assess the bioavailability of acyclovir delivered via the intranasal mucoadhesive gel compared to intravenous administration.

Main Methods:

• Formulation of multilamellar and unilamellar liposomes containing acyclovir.
• Partitioning of acyclovir liposomes into a poly-N-vinyl-2-pyrrolidone (PVP) mucoadhesive gel.
• Determination of entrapment efficiency for both liposomal types.
• In vivo assessment of acyclovir bioavailability using the nasal mucoadhesive gel compared to an intravenous route.

Main Results:

• Entrapment efficiency was higher in multilamellar liposomes (43.2% ± 0.83) than unilamellar liposomes (21% ± 1.01).
• Acyclovir bioavailability from the nasal mucoadhesive gel reached 60.72% relative to the intravenous route.
• The combination of acyclovir liposomes and mucoadhesive gel facilitated prolonged drug contact and direct nasal absorption.

Conclusions:

• Acyclovir-loaded liposomes incorporated into a nasal mucoadhesive gel represent a promising strategy for enhanced systemic drug delivery.
• This formulation improves drug contact time and absorption efficiency via the nasal mucosa.
• Intranasal liposomal acyclovir offers a viable alternative for achieving significant systemic bioavailability.