The College of Pharmacy discussed the PhD dissertation entitled “Lomustine Loaded Solusome as Sprayable Nose to Brain: Preparation and In-Vitro/In-Vivo Evaluation” by the student Ihab Dahham Hammoodi and the supervisor, Professor Dr. Nawal Ayash Rajab, at the Pharmaceutics Department.
The study aimed to achieve targeted and site-specific delivery of lomustine (LOM) to brain tumors through formulation and evaluation of a spray-based drug delivery system utilizing LOM loaded nanovesicle carriers for nose-to-brain drug delivery.
The study included preparation of LOM loaded nanovesicle carriers for spray-based drug delivery using the thin-film hydration method, followed by ultrasonication, employing LOM, cholesterol, Soluplus, and different phosphatidylcholine sources. Thirty formulations were evaluated in terms of particle size (PS), polydispersity index (PDI), entrapment efficiency (EE%), and drug loading percentage (DL%). Additional characterization studies were conducted on the optimized formulation.
The results showed that the optimized formulation exhibited a PS of 94.3 ± 2.39 nm, a PDI of 0.231 ± 0.005, an EE% of 85.88 ± 0.77%, and a zeta potential of −32.16 ± 1.4 mV. In vitro studies revealed that the optimized formulation achieved a cumulative drug release of 93% after 120 minutes, which was significantly higher than that of the pure LOM solution. Solid-state analyses demonstrated complete encapsulation of LOM in an amorphous state within the lipid–polymer matrix, with excellent compatibility between the drug and the excipients. Furthermore, ex vivo studies demonstrated a 3.3-fold enhancement in permeation flux across the nasal mucosa, accompanied by a reduction in lag time. In vivo studies revealed that the formulation achieved a brain drug concentration 2.2 times higher than that obtained following intravenous administration, indicating enhanced brain-targeting ability. Histopathological examination confirmed the biocompatibility of the formulation with the nasal mucosa. Additionally, the formulation maintained its stability at temperatures ranging from 2 to 8°C for three months.
The study recommended incorporating the selected formulation into different gel bases, such as poloxamer, chitosan, and carbopol, to investigate their effects on drug release and permeation. It also recommended incorporating the selected formulation into other nasal spray delivery systems, such as Precision Olfactory Delivery (POD) devices, followed by further investigations. Moreover, long-term stability studies of the prepared formulation and estimation of the expiry date were recommended.
