Figure - available from: International Journal of Nanomedicine
This content is subject to copyright. Terms and conditions apply.
(A) Schematic illustration of the determination of hydroxy-α-sanshool nano-liposomes release. (B) The continuous Release curve of HAS and HAS-LP in vitro. (C) Release model of the group of HAS. (D) Release model of the group of HAS-LP.
Source publication
Purpose
Hydroxy-α-sanshool (HAS) improves cognitive dysfunction, but its structural instability has limited its clinical application. The present study was conducted to investigate the optimal formulation of hydroxy-α-sanshool liposomes (HAS-LPs) and its effect on ameliorating learning and memory disorders in an Alzheimer’s disease (AD) model.
Met...
Citations
... Oral administration has been one of the most preferred routes for drug delivery because of its safety and convenience, which could allow more flexibility in dosing frequency and improve patient compliance [13]. Nowadays, different delivery carriers for HAS have been reported, such as nanostructured lipid carriers and liposomes, which could enhance the solubility, stability or bioavailability of HAS [14,15]. Although these delivery carriers for HAS possesses various advantages, the oral delivery of HAS remains a major challenge and often causes a decrease in oral bioavailability because of the rapid degradation in the complex gastrointestinal environment [10]. ...
Background:
Hydroxy-α-Sanshool (HAS) possesses various pharmacological properties, such as analgesia and regulating gastrointestinal function. However, the low oral bioavailability of HAS has limited its oral delivery in clinical application.
Methods and results:
To enhance its oral bioavailability, a nanocomposite delivery system based on chitosan (CH, as the polycation) and sodium alginate (SA, as the polyanion) was prepared using a layer-by-layer coating technique. The morphology, thermal behavior and Fourier transform infrared spectrum (FTIR) showed that the obtained sodium alginate/chitosan-coated HAS-loaded liposomes (SA/CH-HAS-LIP) with core-shell structures have been successfully covered with polymers. When compared with HAS-loaded liposomes (HAS-LIP), SA/CH-HAS-LIP displayed obvious pH sensitivity and a sustained-release behavior in in vitro studies, which fitted well to Weibull model. In vivo, the half-life of HAS from SA/CH-HAS-LIP remarkably extended after oral administration compared to the free drug. Additionally, it allowed a 4.6-fold and 4.2-fold increase in oral bioavailability, respectively, compared with free HAS and HAS-LIP.
Conclusions:
SA/CH-HAS-LIP could be a promising release vehicle for the oral delivery of HAS to increase its oral bioavailability.
... Developed liposomes were not toxic to the mouse nasal mucosa and effectively improved learning memory deficits induced by d-galactose and protected mouse neuronal cells of the hippocampus. The authors concluded that these hydroxy-α-sanshool liposomes might be used for the management of AD [47]. ...
Diseases related to the brain are causing a huge problem worldwide. Different drug formulations are available for the management of brain-related disorders, but due to less drug availability for the brain and non-specificity, it becomes difficult to completely cure life-threatening brain disorders. The blood-brain barrier (BBB) restricts the entry of drug molecules/drug-loaded carriers because of the presence of various efflux transporters and drug inactivating enzymes. Researchers have identified an intranasal route for direct delivery to the brain, bypassing BBB. Nanotechnology-enabled lipid-based drug carrier systems have shown potential for the management of brain diseases through nose-to-brain delivery. Liposomes are the most extensively investigated carrier systems because of biocompatibility, controlled release characteristics, easy surface modification, and biodegradability. This chapter highlights the important aspects of nose-to-brain delivery and strategies for enhancing the availability of drugs through liposomes in the management of different brain-related diseases.
... Entrapment efficiency is the ratio of the drug or gene entrapped in the liposomes to the total amount used in the preparation. Entrapment efficiency is usually reported for small-molecule drugs [67,83], peptides [40], and proteins [84] encapsulated in liposomes. ...
... Hydroxy-α-sanshool, an unsaturated fatty acid amide found in Zanthoxylum bungeanum, possesses anti-AD activity. In a recent study, Li et al. loaded this compound into liposomes to improve its stability and deliver it to the brain via IN administration [83]. The drug-loaded liposomes caused almost no damage to the nasal mucosa, indicating the safety of the developed liposomes. ...
... IN liposomes can effectively improve the drug and gene accumulation in the brain compared to free drugs (oral and IN) or oral formulations. In many cases, the AUC plasma also increased [39,42,83,120,124]. Interestingly, liposomes can cross the BBB and enter the brain after being absorbed into the systemic circulation from the nasal cavity. ...
Liposomes are safe, biocompatible, and biodegradable spherical nanosized vesicles produced from cholesterol and phospholipids. Recently, liposomes have been widely administered intranasally for systemic and brain delivery. From the nasal cavity, liposome-encapsulated drugs and genes enter the systemic circulation primarily via absorption in the respiratory region, whereas they can be directly transported to the brain via the olfactory pathway. Liposomes can protect drugs and genes from enzymatic degradation, increase drug absorption across the nasal epithelium, and prolong the residence time in the nasal cavity. Intranasal liposomes are also a potential approach for vaccine delivery. Liposomes can be used as a platform to load antigens and as vaccine adjuvants to induce a robust immune response. With the recent interest in intranasal liposome formulations, this review discusses various aspects of liposomes that make them suitable for intranasal administration. We have summarized the latest advancements and applications of liposomes and evaluated their performance in the systemic and brain delivery of drugs and genes administered intranasally. We have also reviewed recent advances in intranasal liposome vaccine development and proposed perspectives on the future of intranasal liposomes.
... De Barros et al. [129] proposed developing and optimizing ghrelin-carrying liposomes using the quality by design approach. The study also used the lipid film rehydration protocol, but two post-formation processes were evaluated: membrane extrusion and high-pressure homogenization. ...
... Lipid film rehydration/ extrusion -72.0-140.0 - [123] Anionic/ thermoresponsive Gel [129] copolymers, showing higher stability and charge retention efficiency than liposomes. Some commonly used polymers include polyethylene glycols and polydimethylsiloxanes. ...
Objectives
Nanotechnology-based nasal delivery systems have gained interest as a way of overcoming low drug bioavailability, limited brain exposure, fast metabolism and elimination, high doses, and unwanted side effects. The main benefits of intranasal administration include the non-invasive method, easy accessibility, porous epithelial barrier and highly vascularized tissue. However, it is imperative to identify interactions between the materials used and the nasal biological environment to ensure proper release.
Methods
Specific factors have been considered to comply with the strict nasal drug administration criteria. Given the broad interest in the nasal drug delivery system, this review summarizes ways to develop formulations for intranasal drug delivery and the main biopharmaceutical challenges.
Key findings
We have examined principal factors in nasal administration, such as physiological aspects of the nose, drug and biopharmaceutical properties, formulation properties, and nasal devices for drug delivery.
Conclusions
This review highlights new insights into different nanotechnology-based approaches for intranasal use and focuses on recent developments in topical nasal drug delivery systems (DDS), outlining the advantages and limitations of each system. The present article confines itself to research and novel concepts and the different strategies developed to increase bioavailability, safety, and a route to brain delivery.
... Liposomes were not significantly toxic to the nasal mucosa and effectively alleviated D-galactose-induced learning memory deficits and protected mouse hippocampal neuronal cells Li et al., 2022 Imatinib Mesylate ...
Alzheimer's disease (AD) is a kind of dementia that creates serious challenges for sufferers' memory, thinking, and behavior. It commonly targeting the aging population and decay the brain cells, despite attempts have been performed to enhance AD diagnostic and therapeutic techniques. Hence, AD remains incurable owing to its complex and multifactorial consequences and still there is lack of appropriate diagnostics/therapeutics option for this severe brain disorder. Therefore, nanotechnology is currently bringing new tools and insights to improve the previous knowledge of AD and ultimately may provide a novel treatment option and a ray of hope to AD patients. Here in this review, we highlighted the nanotechnologies-based findings for AD, in both diagnostic and therapeutic aspects and explained how advances in the field of nanotechnology/nanomedicine could enhance patient prognosis and quality of life. It is highly expected these emerging technologies could bring a research-based revolution in the field of neurodegenerative disorders and may assist their clinical experiments and develop an efficacious drug for AD also. The main aim of review is to showcase readers the recent advances in nanotechnology-based approaches for treatment and diagnosing of AD.
... Sensasi trigeminal andaliman disebabkan oleh kandungan alkilamida tidak jenuh yang lebih dikenal sebagai sanshool (Wijaya, 2000). Selain memberikan sensasi trigeminal yang unik ketika dikonsumsi, sanshool juga dilaporkan dapat memberikan efek fisiologis aktif seperti melindungi kulit dari kerusakan oleh radiasi ultraviolet (Hao et al., 2019), mencegah obesitas dan mengurangi lemak , mencegah kerusakan sel dari reaksi oksidatif (Li et al., 2020), mencegah penurunan fungsi kognitif , serta memiliki potensial sebagai bahan anti-aging dalam kosmetik (Kim et al., 2021;Zeng et al., 2019) dan terapi penyakit Alzheimer (Li et al., 2022;Liu et al., 2022). ...
Sanshool compounds are the trigeminal active compounds in andaliman (Zanthoxylum acantho-podium DC) with a numbing and tingling sensation. The analysis of such compounds is usually done through HPLC approach; however, limited studies have reported that the analysis of such compounds could be conducted with Gas Chromatography-Mass Spectrometry (GC-MS). This method could save research time and funding by analyzing both sanshools and volatiles simultaneously, which would describe the complete profile of andaliman flavor compounds. This study aimed to confirm the potency of GC-MS in analyzing sanshool compounds and to utilize this method in studying the impact of different drying methods towards andaliman trigeminal active compounds. Andaliman was dried with five drying methods (sun, sunshade, air, oven, and freeze-drying) and was macerated with chloroform, concentrated, and analyzed with GC-MS. The results of this study showed that GC-MS was able to analyze sanshool compounds efficiently. Drying had no statistically significant impact on sanshool quantities extracted from andaliman. Fresh andaliman contained 0.69 % (dry weight basis) of α-sanshool, the main sanshool in andaliman. On the other hand, dried andaliman contained 0.80-1.08% of α-sanshool (dry weight basis). As oven drying managed to produce andaliman with a similar concentration of α-sanshool at a faster time and more affordable cost than other drying methods, oven drying was suggested as the ideal drying method to extend the shelf life of andaliman.
Liposomes—microscopic phospholipid bubbles with bilayered membrane structure—have been a focal point in drug delivery research for the past 30 years. Current liposomes possess a blend of biocompatibility, drug loading efficiency, prolonged circulation and targeted delivery. Tailored liposomes, varying in size, charge, lipid composition, and ratio, have been developed to address diseases in specific organs, thereby enhancing drug circulation, accumulation at lesion sites, intracellular delivery, and treatment efficacy for various organ‐specific diseases. For further successful development of this field, this review summarized liposomal strategies for targeting different organs in series of major human diseases, including widely studied cardiovascular diseases, liver and spleen immune diseases, chronic or acute kidney injury, neurodegenerative diseases, and organ‐specific tumors. It highlights recent advances of liposome‐mediated therapeutic agent delivery for disease intervention and organ rehabilitation, offering practical guidelines for designing organ‐targeted liposomes.
This article is categorized under: Therapeutic Approaches and Drug Discovery > Emerging Technologies
Biology‐Inspired Nanomaterials > Lipid‐Based Structures
The brain is a highly complex interconnected neuronal network with a specialized blood–brain barrier (BBB). The BBB is a diffusion barrier crucial for protecting normal brain function by blocking dangerous compounds from crossing the bloodstream to the brain; only small molecules can cross the BBB. However, brain diseases, such as Alzheimer’s disease, Parkinson’s disease, seizures, multiple sclerosis, stroke, and brain cancers, are some of the most dominant, traumatic, and nevertheless poorly treated diseases. The development of drug delivery systems for brain disorders has had the poorest achievement rates as compared to other therapeutic areas. Exosomes are extracellular nanovesicles consisting of proteins, messenger RNAs, and microRNAs. They are the most prominent mediators of intercellular communication, regulating, instructing, and re-educating their surrounding environment as well as targeting different organs through their surface modifications. Exosomes are secreted by blood cells and endothelial cells directly into the blood circulation in response to CNS pathological conditions. Secreted exosomes express their markers and offer to track their cellular origin, in addition to making them useful for diagnostic purposes and disease treatments. In this book chapter, we have focused on the biogenesis of exosomes along with their functions and contribution to the treatment of brain disorders. We end this chapter with an account of diagnostic tools and their future prospects with respect to diseases associated with the central nervous system.
