Direct Brain Targeted Nanostructured Lipid Carriers for Sustained Release of Schizophrenic Drug: Formulation, Characterization and Pharmacokinetic Studies

Sivadasu, Praveen; Gowda, Devagowda Vishakante; Subramani, Nithin Kundachira; Vishweshwaraiah, Bhavya Malgur; Shivanna, Sachhidananda; Hatna, Siddaramaiah

doi:10.5530/ijper.54.1.9

Cited by 11 publications

(4 citation statements)

References 41 publications

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“…The QF blood–brain ratio showed a 10-fold increase for NLCs administered through the nasal route (in comparison to the intravenous route), supporting retention of the drug at the desired site. The study supports a potential nose-to-brain transport of QF-NLC for the effective management of schizophrenia by circumventing the BBB [ 165 ].…”

Section: Lipid-based Nanocarrier Systems For Cns Deliverysupporting

confidence: 70%

Potential of Lipid-Based Nanocarriers against Two Major Barriers to Drug Delivery—Skin and Blood–Brain Barrier

et al. 2023

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Over the past few years, pharmaceutical and biomedical areas have made the most astounding accomplishments in the field of medicine, diagnostics and drug delivery. Nanotechnology-based tools have played a major role in this. The implementation of this multifaceted nanotechnology concept encourages the advancement of innovative strategies and materials for improving patient compliance. The plausible usage of nanotechnology in drug delivery prompts an extension of lipid-based nanocarriers with a special reference to barriers such as the skin and blood–brain barrier (BBB) that have been discussed in the given manuscript. The limited permeability of these two intriguing biological barriers restricts the penetration of active moieties through the skin and brain, resulting in futile outcomes in several related ailments. Lipid-based nanocarriers provide a possible solution to this problem by facilitating the penetration of drugs across these obstacles, which leads to improvements in their effectiveness. A special emphasis in this review is placed on the composition, mechanism of penetration and recent applications of these carriers. It also includes recent research and the latest findings in the form of patents and clinical trials in this field. The presented data demonstrate the capability of these carriers as potential drug delivery systems across the skin (referred to as topical, dermal and transdermal delivery) as well as to the brain, which can be exploited further for the development of safe and efficacious products.

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Section: Lipid-based Nanocarrier Systems For Cns Deliverysupporting

confidence: 70%

Potential of Lipid-Based Nanocarriers against Two Major Barriers to Drug Delivery—Skin and Blood–Brain Barrier

et al. 2023

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“…Their innovative approach, involving the modification of nanoparticles with borneol, demonstrated enhanced brain delivery, showcasing the versatility of lipid-based carriers in optimizing intranasal drug delivery. Direct brain-targeted nanostructured lipid carriers for the sustained release of a schizophrenic drug were developed by Sivadasu et al [ 70 ]. The study encompassed formulation development, characterization, and pharmacokinetic evaluations, establishing the potential of lipid-based carriers in sustaining drug release and optimizing therapeutic outcomes for psychiatric disorders.…”

Section: Discussionmentioning

confidence: 99%

Navigating the Nose-to-Brain Route: A Systematic Review on Lipid-Based Nanocarriers for Central Nervous System Disorders

Agosti,

Zeppieri,

Antonietti

et al. 2024

Pharmaceutics

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Background: The blood–brain barrier (BBB) regulates brain substance entry, posing challenges for treating brain diseases. Traditional methods face limitations, leading to the exploration of non-invasive intranasal drug delivery. This approach exploits the direct nose-to-brain connection, overcoming BBB restrictions. Intranasal delivery enhances drug bioavailability, reduces dosage, and minimizes systemic side effects. Notably, lipid nanoparticles, such as solid lipid nanoparticles and nanostructured lipid carriers, offer advantages like improved stability and controlled release. Their nanoscale size facilitates efficient drug loading, enhancing solubility and bioavailability. Tailored lipid compositions enable optimal drug release, which is crucial for chronic brain diseases. This review assesses lipid nanoparticles in treating neuro-oncological and neurodegenerative conditions, providing insights for effective nose-to-brain drug delivery. Methods: A systematic search was conducted across major medical databases (PubMed, Ovid MEDLINE, and Scopus) up to 6 January 2024. The search strategy utilized relevant Medical Subject Heading (MeSH) terms and keywords related to “lipid nanoparticles”, “intranasal administration”, “neuro-oncological diseases”, and “neurodegenerative disorders”. This review consists of studies in vitro, in vivo, or ex vivo on the intranasal administration of lipid-based nanocarriers for the treatment of brain diseases. Results: Out of the initial 891 papers identified, 26 articles met the eligibility criteria after a rigorous analysis. The exclusion of 360 articles was due to reasons such as irrelevance, non-reporting selected outcomes, the article being a systematic literature review or meta-analysis, and lack of method/results details. This systematic literature review, focusing on nose-to-brain drug delivery via lipid-based nanocarriers for neuro-oncological, neurodegenerative, and other brain diseases, encompassed 60 studies. A temporal distribution analysis indicated a peak in research interest between 2018 and 2020 (28.3%), with a steady increase over time. Regarding drug categories, Alzheimer’s disease was prominent (26.7%), followed by antiblastic drugs (25.0%). Among the 65 drugs investigated, Rivastigmine, Doxorubicin, and Carmustine were the most studied (5.0%), showcasing a diverse approach to neurological disorders. Notably, solid lipid nanoparticles (SLNs) were predominant (65.0%), followed by nanostructured lipid carriers (NLCs) (28.3%), highlighting their efficacy in intranasal drug delivery. Various lipids were employed, with glyceryl monostearate being prominent (20.0%), indicating preferences in formulation. Performance assessment assays were balanced, with in vivo studies taking precedence (43.3%), emphasizing the translation of findings to complex biological systems for potential clinical applications. Conclusions: This systematic review reveals the transformative potential of intranasal lipid nanoparticles in treating brain diseases, overcoming the BBB. Positive outcomes highlight the effectiveness of SLNs and NLCs, which are promising new approaches for ailments from AD to stroke and gliomas. While celebrating progress, addressing challenges like nanoparticle toxicity is also crucial.

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“…Results demonstrated the superiority of the developed quetiapine-loaded NLC formulation as a stable drug-delivery system. Overall, it was concluded that the NLCs provide a promising approach to enhance the transportation of quetiapine to the brain, hence addressing the treatment of bipolar disorder [ 132 ]. The potential of NLCs in delivering diazepam-loaded NLCs by intranasal delivery and the possible toxicity were reported.…”

Section: Nanoparticles For Nose-to-brain Drug Deliverymentioning

confidence: 99%

Nasal Delivery to the Brain: Harnessing Nanoparticles for Effective Drug Transport

Gandhi,

Shastri,

Shah

et al. 2024

Pharmaceutics

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The nose-to-brain drug-delivery system has emerged as a promising strategy to overcome the challenges associated with conventional drug administration for central nervous system disorders. This emerging field is driven by the anatomical advantages of the nasal route, enabling the direct transport of drugs from the nasal cavity to the brain, thereby circumventing the blood–brain barrier. This review highlights the significance of the anatomical features of the nasal cavity, emphasizing its high permeability and rich blood supply that facilitate rapid drug absorption and onset of action, rendering it a promising domain for neurological therapeutics. Exploring recent developments and innovations in different nanocarriers such as liposomes, polymeric nanoparticles, solid lipid nanoparticles, dendrimers, micelles, nanoemulsions, nanosuspensions, carbon nanotubes, mesoporous silica nanoparticles, and nanogels unveils their diverse functions in improving drug-delivery efficiency and targeting specificity within this system. To minimize the potential risk of nanoparticle-induced toxicity in the nasal mucosa, this article also delves into the latest advancements in the formulation strategies commonly involving surface modifications, incorporating cutting-edge materials, the adjustment of particle properties, and the development of novel formulations to improve drug stability, release kinetics, and targeting specificity. These approaches aim to enhance drug absorption while minimizing adverse effects. These strategies hold the potential to catalyze the advancement of safer and more efficient nose-to-brain drug-delivery systems, consequently revolutionizing treatments for neurological disorders. This review provides a valuable resource for researchers, clinicians, and pharmaceutical-industry professionals seeking to advance the development of effective and safe therapies for central nervous system disorders.

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Direct Brain Targeted Nanostructured Lipid Carriers for Sustained Release of Schizophrenic Drug: Formulation, Characterization and Pharmacokinetic Studies

Cited by 11 publications

References 41 publications

Potential of Lipid-Based Nanocarriers against Two Major Barriers to Drug Delivery—Skin and Blood–Brain Barrier

Potential of Lipid-Based Nanocarriers against Two Major Barriers to Drug Delivery—Skin and Blood–Brain Barrier

Navigating the Nose-to-Brain Route: A Systematic Review on Lipid-Based Nanocarriers for Central Nervous System Disorders

Nasal Delivery to the Brain: Harnessing Nanoparticles for Effective Drug Transport

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