article · Drug Delivery
Delivering medication to the brain to treat stroke damage is difficult because the blood-brain barrier restricts foreign molecules from entering. To address this challenge, solid lipid nanoparticles were formulated and optimised to deliver the drug valsartan directly to the brain. The formulation process evaluated how lipid concentration, surfactant concentration, and homogenisation speed affected nanoparticle size, surface charge, drug entrapment, and release rates. The resulting spherical nanoparticles provided sustained drug release over 72 hours, with valsartan successfully encapsulated in an amorphous state. In vivo tests showed that administering the optimised formulation through the intranasal route successfully transported valsartan into the brain, performing significantly better than a standard valsartan solution as verified by fluorescence imaging. This approach presents a viable method for targeted, sustained delivery to mitigate ischaemic brain damage.
Strokes cause severe brain damage, but treating them remains difficult because the protective blood-brain barrier prevents most drugs from reaching neural tissue. Using lipid nanoparticles to deliver valsartan via the nasal cavity allows the drug to access the brain while releasing it slowly. This strategy could improve recovery outcomes for stroke patients and reduce the required frequency of medication doses.
This work represents early-stage, in vivo laboratory research that could enable pharmaceutical manufacturers to develop intranasal delivery systems for stroke therapy. Targeted users would ultimately be medical professionals managing ischaemia-induced brain injury. The technology is in pre-clinical development and requires formal clinical trials, pharmacokinetic profiling, and manufacturing scale-up before it can be translated into a commercial drug product.
AI-generated from the published abstract. Always read the original work before citing.
The brain is a vital organ that is protected from the general circulation and is distinguished by the presence of a relatively impermeable blood brain barrier (BBB). Blood brain barrier prevents the entry of foreign molecules. The current research aims to transport valsartan (Val) across BBB utilizing solid lipid nanoparticles (SLNs) approach to mitigate the adverse effects of stroke. Using a 32-factorial design, we could investigate and optimize the effect of several variables in order to improve brain permeability of valsartan in a target-specific and sustained-release manner, which led to alleviation of ischemia-induced brain damage. The impact of each of the following independent variables was investigated: lipid concentration (% w/v), surfactant concentration (% w/v), and homogenization speed (RPM) on particle size, zeta potential (ZP), entrapment efficiency (EE) %, and cumulative drug release percentage (CDR) %. TEM images revealed a spherical form of the optimized nanoparticles, with particle size (215.76 ± 7.63 nm), PDI (0.311 ± 0.02), ZP (-15.26 ± 0.58 mV), EE (59.45 ± 0.88%), and CDR (87.59 ± 1.67%) for 72 hours. SLNs formulations showed sustained drug release, which could effectively reduce the dose frequency and improve patient compliance. DSC and X-ray emphasize that Val was encapsulated in the amorphous form. The in-vivo results revealed that the optimized formula successfully delivered Val to the brain through intranasal rout as compared to a pure Val solution and evidenced by the photon imaging and florescence intensity quantification. In a conclusion, the optimized SLN formula (F9) could be a promising therapy for delivering Val to brain, alleviating the negative consequences associated with stroke.
This page summarises published work. The authoritative version sits with the publisher.
DOI: 10.1080/10717544.2023.2179127
Is something wrong with this record? Report it or request removal.
Discussion
Have you built on this work, tried to replicate it, or seen it applied in practice? Share what you know. Verified researchers and MARATTO™ domain experts can open a discussion, and any member can reply. Contributions are reviewed before they appear.
No discussion yet. Open the first thread.
New to MARATTO™? Create a free account.
