Surface-modified liposomal in-situ nasal gel enhances brain targeting of berberine hydrochloride for Alzheimer’s therapy: optimization and in vivo studies DOI

Sejal Bahndare,

Dyandevi Mathure,

Hemantkumar Ranpise

et al.

Journal of Liposome Research, Journal Year: 2024, Volume and Issue: unknown, P. 1 - 18

Published: Nov. 25, 2024

This work aimed to formulate surface-modified berberine hydrochloride (BER)-loaded liposomes containing

Language: Английский

Development of Atomoxetine-Loaded NLC In Situ Gel for Nose-to-Brain Delivery: Optimization, In Vitro, and Preclinical Evaluation DOI Creative Commons
Dibyalochan Mohanty, Omar Awad Alsaidan,

Ameeduzzafar Zafar

et al.

Pharmaceutics, Journal Year: 2023, Volume and Issue: 15(7), P. 1985 - 1985

Published: July 20, 2023

The present study investigates the brain-targeted efficiency of atomoxetine (AXT)-loaded nanostructured lipid carrier (NLC)-laden thermosensitive in situ gel after intranasal administration. AXT-NLC was prepared by melt emulsification ultrasonication method and optimized using Box–Behnken design (BBD). formulation (AXT-NLC) exhibited particle size PDI, zeta potential, entrapment (EE) 108 nm, 0.271, −42.3 mV, 84.12%, respectively. morphology found to be spherical, as confirmed SEM analysis. DSC results displayed that AXT encapsulated within NLC matrix. Further, (AXT-NLC13) incorporated into a poloxamer 407 carbopol gelling agent evaluated for different parameters. (AXT-NLC13G4) showed excellent viscosity (2532 ± 18 Cps) at 37 °C formed 28–34 °C. AXT-NLC13-G4 sustained release (92.89 3.98% 12 h) compared pure (95.47 2.76% 4 h). permeation flux through goat nasal mucosa from 504.37 µg/cm2·h 232.41 µg/cm2·h, intranasally significantly higher absolute bioavailability (1.59-fold higher) than intravenous 51.91% BTP (28.64%) when administered via same route (intranasally). BTE (207.92%) (140.14%) intranasally, confirming high amount reached brain. With disrupted performance induced L-methionine, (p < 0.05) better activity well donepezil (standard). finding concluded is novel improvement brain delivery requires further investigation more justification.

Language: Английский

Citations

27

Design of experiment (DoE) as a quality by design (QbD) tool to optimise formulations of lipid nanoparticles for nose-to-brain drug delivery DOI
Aline de Alcântara Correia, João Nuno Moreira, José Manuel Sousa Lobo

et al.

Expert Opinion on Drug Delivery, Journal Year: 2023, Volume and Issue: 20(12), P. 1731 - 1748

Published: Oct. 31, 2023

The nose-to-brain route has been widely investigated to improve drug targeting the central nervous system (CNS), where lipid nanoparticles (solid - SLN and nanostructured carriers NLC) seem promising, although they should meet specific criteria of particle size (PS) <200 nm, polydispersity index (PDI) <0.3, zeta potential (ZP) ~|20| mV encapsulation efficiency (EE) >80%. To optimize NLC formulations, design experiment (DoE) recommended as a quality by (QbD) tool.

Language: Английский

Citations

14

Design of experiment (DoE) of mucoadhesive valproic acid-loaded nanostructured lipid carriers (NLC) for potential nose-to-brain application DOI Creative Commons
António Correia, Inês Costa, Rui Silva

et al.

International Journal of Pharmaceutics, Journal Year: 2024, Volume and Issue: 664, P. 124631 - 124631

Published: Aug. 29, 2024

Epilepsy is a highly prevalent neurological disease and valproic acid (VPA) used as first-line chronic treatment. However, this drug has poor oral bioavailability, which requires the administration of high doses, resulting in adverse effects. Alternative routes VPA have therefore been investigated, such nose-to-brain route, allows to be transported directly from nasal cavity brain. Here, use nanostructured lipid carriers (NLC) encapsulate drugs administered proved advantageous. The aim work was optimise mucoadhesive formulation VPA-loaded NLC for intranasal improve treatment epilepsy. Design Experiment (DoE) formulation, starting with component optimisation using Mixture (MD), followed by manufacturing process parameters Central Composite (CCD). optimised had particle size 76.1 ± 2.8 nm, polydispersity index 0.190 0.027, zeta potential 28.1 2.0 mV an encapsulation efficiency 85.4 0.8%. vitro release study showed 50 % after 6 h 100 24 h. biocompatibility experiments various cell lines shown that safe up 75 µg/mL, neuronal (SH-SY5Y), (RPMI 2650) hepatic (HepG2) cells. Finally, interaction mucus investigated properties were observed. results suggest may promising alternative promote targeting brain, thereby improving bioavailability minimising

Language: Английский

Citations

4

Optimized Hesperidin-Loaded Lipid Nanoparticles with Tea Tree Oil for Enhanced Wound Healing: Formulation, Characterization, and Evaluation DOI Creative Commons
Borros Arneth, Rehab Abdelmonem, Mohamed A. El-Nabarawi

et al.

Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(3), P. 290 - 290

Published: Feb. 20, 2025

Objectives: This study aimed to develop hesperidin solid lipid nanoparticles (HESP-SLNs) enhance their stability, solubility, and sustained release for wound healing; further enhancement was achieved through prepared nanostructured carriers (HESP-NLCs) using Tea Tree Oil (TTO) explore synergistic efficacy. Methods: A factorial design of 24 trials established evaluate the influence type (X1), conc (%) (X2), surfactant (X3), sonication amplitude (X4) HESP-SLNs on particle size (nm) (Y1), polydispersibility index (Y2), zeta potential (Y3), encapsulation efficiency (Y4). The optimized formula selected utilizing Design Expert® software version 13, which additionally enhanced by preparing TTO-loaded HESP-NLCs. In vitro release, Raman spectroscopy, transmission electron microscopy were carried out both nanoparticles. Cytotoxicity, in vivo wound-healing assessments, skin irritancy tests performed performance TTO-incorporated HESP-NLCs compared HESP-SLNs. Results: demonstrated PS (280 ± 1.35 nm), ZP (−39.4 0.92 mV), PDI (0.239 0.012), EE% (88.2 2.09%). NLCs Q6% (95.14%) vs. (79.69%), SLNs showed superior antimicrobial Both exhibited spherical morphology compatibility between HESP excipients. highest closure percentage, supported histological analysis inflammatory biomarker outcomes. Cytotoxicity evaluation 87% cell viability untreated HSF cells, test confirmed safety NLCs. Conclusions: are promising candidates exhibiting capabilities, making them a therapeutic option cutaneous management.

Language: Английский

Citations

0

Crosslinked Chitosan Nanoparticles with Muco-Adhesive Potential for Intranasal Delivery Applications DOI Open Access
Mariacristina Gagliardi, Sara Chiarugi, Chiara De Cesari

et al.

International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 24(7), P. 6590 - 6590

Published: April 1, 2023

Intranasal drug delivery is convenient and provides a high bioavailability but requires the use of mucoadhesive nanocarriers. Chitosan well-established polymer for applications can suffer from poor cytocompatibility stability upon administration. In this work, we present method to obtain stable cytocompatible crosslinked chitosan nanoparticles. We used 2,6-pyridinedicarboxylic acid as biocompatible crosslinker compared obtained particles with those prepared by ionotropic gelation using sodium tripolyphosphate. Nanoparticles were tested evaluate size surface charge, well their in storage conditions (4 °C), at nasal cavity temperature (32 body (37 °C). The nanoparticles showed around 150 nm charge 10.3 mV ± 0.9 mV, both compatible intranasal Size parameters did not significantly vary over time, indicating good these finally vitro SHSY5Y human neuroblastoma RPMI 2650 epithelial cells, positive results. conclusion, proposed synthetic system shows an interesting potential carrier delivery.

Language: Английский

Citations

9

Xanthan-Gum/Pluronic-F-127-Based-Drug-Loaded Polymeric Hydrogels Synthesized by Free Radical Polymerization Technique for Management of Attention-Deficit/Hyperactivity Disorder DOI Creative Commons
Muhammad Suhail,

I-Hui Chiu,

Yi-Ru Lai

et al.

Gels, Journal Year: 2023, Volume and Issue: 9(8), P. 640 - 640

Published: Aug. 8, 2023

Smart and intelligent xanthan gum/pluronic F-127 hydrogels were fabricated for the controlled delivery of atomoxetine HCl. Different parameters such as DSC, TGA, FTIR, XRD, SEM, drug loading, porosity, swelling index, release, kinetics modeling appraised prepared matrices hydrogels. FTIR confirmed successful synthesis hydrogel, while TGA DSC analysis indicated that thermal stability reagents was improved after polymerization technique. SEM revealed hard surface XRD a reduction in crystallinity reagents. High gel fraction achieved with high incorporated contents polymers monomer. An increase swelling, release observed concentrations gum acrylic acid, whereas Pluronic showed opposite effect. A negligible index shown at pH 1.2 4.6 greater 7.4, indicating pH-responsive nature designed Furthermore, higher found 7.4 compared to 4.6, respectively. The first order followed by hydrogel formulations. Thus, it is signified from discussion smart have potential control HCl colon an extended period time.

Language: Английский

Citations

9

Multifaceted Applications of Solid Lipid: A Comprehensive Review DOI
Chinam Niranjan Patra, Kartikesh Sahu, R. K. Singha

et al.

Deleted Journal, Journal Year: 2024, Volume and Issue: 2(2), P. 834 - 860

Published: Feb. 5, 2024

Lipids originate from plant and animal sources have significant roles in various fields, like pharmaceuticals, cosmetics, food, paint, leather, agriculture, microfluidics, oil industries. Over the years, with development of technology, different types lipids been synthesized or extracted used based on their industrial need. are heterogeneous group compounds related to fatty acids insoluble water but soluble organic solvents. One category great importance is solid lipids. Solid a type that remain at ambient temperature. In past, were obtained natural they mainly as bulking agents bases for dosage forms. due course time, after industrialization, evolved gained more significance. drug targeting controlled delivery release rate modifiers, solubilizers, stabilizers, permeation enhancers improved biopharmaceutical performance drugs. These also popular diversified applications industries mentioned above. this review, authors selected some Stearic acid, Compritol®ATO 888, Precirol®ATO 5, Glyceryl Monostearate, Witepsol®, Carnauba wax, Softisan®, Cholesterol, Dynasan®, Cetyl palmitate discussed about properties applications.

Language: Английский

Citations

3

Nose to Brain: Exploring the Progress of Intranasal Delivery of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers DOI Creative Commons

Yang Zheng,

Limei Cui,

Haoran Lu

et al.

International Journal of Nanomedicine, Journal Year: 2024, Volume and Issue: Volume 19, P. 12343 - 12368

Published: Nov. 1, 2024

The intranasal (IN) route of drug delivery can effectively penetrate the blood-brain barrier and deliver drugs directly to brain for treatment central nervous system (CNS) disorders via intra-neuronal or extra-neuronal pathways. This approach has several advantages, including avoidance first-pass metabolism, high bioavailability, ease administration, improved patient compliance. In recent years, an increasing number studies have been conducted using encapsulated in solid lipid nanoparticles (SLNs) nanostructured carriers (NLCs), delivering them IN pathway. SLNs are first-generation nanocarriers, known their excellent biocompatibility, drug-loading capacity, remarkable stability. NLCs, regarded as second-generation SLNs, not only retain advantages but also exhibit enhanced stability, preventing leakage during storage. this review, we examined vivo between 2019 2024 that used NLCs address CNS route. By statistical methods evaluate pharmacokinetic parameters, found markedly accumulation targeting within brain. Additionally, pharmacodynamic evaluations indicated method substantially therapeutic effectiveness alleviating symptoms rat models diseases. addition, enhancing efficacy nose-to-brain discussed, well advances clinical trials regarding NLCs.

Language: Английский

Citations

2

Quality by design approach for development and characterization of gabapentin-loaded solid lipid nanoparticles for intranasal delivery: DOI
Mahmut Ozan Toksoy, Fırat Aşır, Mert Can Güzel

et al.

PubMed, Journal Year: 2024, Volume and Issue: 27(7), P. 904 - 913

Published: Jan. 1, 2024

"Quality by Design" (QbD) is a novel approach to product development that involves understanding the and process, as well relationship between critical quality attributes (CQA) process parameters (CPP). This study aimed optimize gabapentin-loaded solid lipid nanoparticle formulation (GP-SLN) using QbD evaluate in vitro ex vivo performance.

Language: Английский

Citations

0

Trastorno por Déficit de Atención/Hiperactividad: persistencia en la adultez DOI Creative Commons
Salvador Pérez-Hernández, I. Paz,

Alejandro Cruz-Rosas

et al.

Vertex Revista Argentina de Psiquiatría, Journal Year: 2024, Volume and Issue: 35(165), P. 67 - 73

Published: Oct. 20, 2024

El trastorno por déficit de atención/hiperactividad (TDAH) es un del neurodesarrollo caracterizado niveles problemáticos inatención, desorganización y/o hiperactividad-impulsividad. Afecta diversos campos la vida paciente como conducta y su desenvolvimiento social académico. TDAH tiene una etiología multifactorial, con implicaciones genéticas, ambientales, socioeconómicas, entre otras. Es principalmente diagnosticado en niños; sin embargo, puede permanecer hasta edad adulta o bien, ser haber pasado desapercibido durante niñez. Existe posibilidad que los síntomas sean compensados ​​al llegar a adultez no producir dificultades, pero cuando hay alteraciones ambientales comorbilidades, pueden evidentes, se enfrenta estrés escolar, laboral dado las cargas trabajo universidad exigente.

Citations

0