Abstract
Curcumin is one of the most promising natural therapeutics for use against Alzheimer’s disease. The major limitations of curcumin are its low oral bioavailability and difficulty in permeating the blood–brain barrier. Therefore, designing a delivery system of curcumin to overcome its limitations must be employed. KLVFF, a peptide known as an amyloid blocker, was used in this study as a targeting moiety to develop a targeted drug delivery system. A prototype of transnasal KLVFF conjugated microemulsions containing curcumin (KLVFF-Cur-ME) for the nose-to-brain delivery was fabricated. The KLVFF-Cur-ME was developed by a titration method. A conjugation of KLVFF was performed through a carbodiimide reaction, and the conjugation efficiency was confirmed by FTIR and DSC technique. KLVFD-Cur-ME was characterized for the drug content, globule size, zeta potential, and pH. A transparent and homogeneous KLVFF-Cur-ME is achieved with a drug content of 80.25% and a globule size of 76.1 ± 2.5 nm. The pH of KLVFF-Cur-ME is 5.33 ± 0.02, indicating non-irritation to nasal tissues. KLVFD-Cur-ME does not show nasal ciliotoxicity. An ex vivo diffusion study revealed that KLVFF-Cur-ME partitions the porcine nasal mucosa through diffusion, following the Higuchi model. This investigation demonstrates the successful synthesis of a bifunctional KLVFF-Cur-ME as a novel prototype to deliver anti-Aβ aggregation via an intranasal administration.
Highlights
Introduction iationsAlzheimer’s disease (AD) contributes to 60–70% of dementia cases, mostly found in the elderly [1]
We propose that binary inhibitors of amyloid aggregation, which have different binding sites, would additively or synergistically inhibit Aβ aggregation
This study describes the synthesis and characterization of surface-modified microemulsions encapsulating curcumin
Summary
Alzheimer’s disease (AD) contributes to 60–70% of dementia cases, mostly found in the elderly [1]. The pathophysiology of Alzheimer’s disease is still not clear, but the beta-amyloid plaque (Aβ) is one of the pathological hallmarks, and is considered a target for treatment. Most therapeutic agents are in the form of tablets and capsules, which cause issues for patients in late-stage AD with swallowing difficulties [3]. These reasons led to the development of various drug formulations administered through routes other than oral. The delivery of the drugs directly to the brain has been shown to improve the efficacy of the treatment [4]. The intranasal administration (IN) of drugs has gained attention because of several advantages, including the direct access of Licensee MDPI, Basel, Switzerland
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