Recent strategies and advances in the fabrication of nano lipid carriers and their application towards brain targeting

Agrawal, Mukta; Saraf, Swarnlata; Saraf, Shailendra; Dubey, Sunil Kumar; Puri, Anu; Patel, Ravish J.; AJAZUDDIN, .; Ravichandiran, V.; Murty, Upadhyayula Suryanarayana; Alexander, Amit

doi:10.1016/j.jconrel.2020.02.020

Cited by 159 publications

(73 citation statements)

References 296 publications

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“…They also have the advantage of reduced toxicity and better biocompatibility compared to polymeric micelles. 14,15 Liposomes, the primary lipid nanocarriers, were applied for drug targeting to the brain despite their limitations that include low drug loading efficiency, rapid clearance through the reticuloendothelial system, and poor stability. Solid lipid nanoparticles (SLN) have been introduced as an alternative to liposomes and polymeric nanocarriers.…”

Section: Introductionmentioning

confidence: 99%

“…In addition, they offer prolongation of drug release and higher stability in comparison to liposomes. 14,16 However, the major disadvantage of SLN is the possibility of drug expulsion and uneven drug incorporation owing to their crystalline structure. Accordingly, nanostructured lipid carriers (NLCs) have been proposed as a second-generation SLN to overcome the aforementioned drawbacks.…”

Section: Introductionmentioning

confidence: 99%

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<p>Optimized Nanostructured Lipid Carriers Integrated into In Situ Nasal Gel for Enhancing Brain Delivery of Flibanserin</p>

Fahmy¹,

Ahmed²,

Badr-Eldin³

et al. 2020

IJN

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Background and Aim: Flibanserin (FLB) is a multifunctional serotonergic agent used for treating hypoactive sexual desire disorder in premenopausal women via oral administration. FLB has a reported limited oral bioavailability of 33% that could be attributed to the drug's first-pass metabolism. In addition, FLB has a pH-dependent solubility that could be a challenging factor for drug dissolution in the body neutral fluid, and consequently, absorption via mucosal barriers. Thus, this work aims at investigating the potential of utilizing nanostructured lipid carriers (NLCs) to overcome the aforementioned drawbacks and to enhance nose-to-brain drug delivery. Methods: Box-Behnken design was applied to explore the impact of solid lipid % (SL%, X 1), liquid lipid % (LL%, X 2), and sonication time (ST, X 3) on particle size. The optimized NLC formulation was characterized and incorporated into gellan gum in situ gel. The prepared gel was subjected to in vitro drug release, in vivo pharmacokinetic performance, and histopathological assessment in rats. Results: Statistical analysis revealed a significant negative effect for both SL% and ST on NLCs size. In contrast, a significant positive effect was observed for the LL%. The optimized formulation showed spherical shape with vesicular size of 114.63 nm. The optimized FLB-NLC in situ gel exhibited adequate stability and enhanced in vitro release compared to raw FLB control gel. The plasma and brain concentrations of the drug after nasal administration in rats increased by more than 3-6-fold, respectively, compared to raw FLB in situ gel. In addition, the histopathological studies revealed the absence of any pathological signs. Conclusion: The aforementioned results highlight the safety of FLB-NLC in situ nasal gel and its potential to improve the drug bioavailability and brain delivery.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

<p>Optimized Nanostructured Lipid Carriers Integrated into In Situ Nasal Gel for Enhancing Brain Delivery of Flibanserin</p>

Fahmy¹,

Ahmed²,

Badr-Eldin³

et al. 2020

IJN

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“…Many efforts have been developed to overcome and reduce these side effects [ 15 ]. The use of nanoparticles (NP) as a delivery vector can be a promising solution, as they are relatively safe, enhance drug bioavailability, decrease blood protein binding and clearance rate [ 16 , 17 ]. Among the most studied nanoparticulate systems, nanostructured lipid carriers (NLCs) are attracting great scientific interest.…”

Section: Introductionmentioning

confidence: 99%

Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid Nanoparticles

et al. 2020

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Tacrine (TAC) was the first FDA approved drug for the treatment of Alzheimer’s disease, resulting in increased memory and enhanced cognitive symptoms in patients. However, long-term therapy presents poor patient compliance associated with undesired side effects such as nausea, vomiting and hepatoxicity. To improve its therapeutic efficacy and decrease toxicity, the use of nanoparticles could be applied as a possible solution to delivery TAC. In this context, a project has been designed to develop a new nanostructured lipid carrier (NLC) as a delivery system for TAC and conjugate TAC and model amphipathic peptide (MAP) to decrease TAC limitations. Different formulations loaded with TAC and TAC + MAP were prepared using a combination of Compritol 888 ATO as the solid lipid and Transcutol HP as the liquid lipid component. Physical characterization was evaluated in terms of particle size, surface charge, encapsulation efficiency and in vitro drug release studies. Particle size distributions within the nanometer range were obtained with encapsulation efficiencies of 72.4% for the TAC and 85.6% for the TAC + MAP conjugate. Furthermore, cytotoxicity of all NLC formulations was determined against neuroblastoma cell line SH-SY5Y. The optimized TAC delivery system revealed low toxicity suggesting this could be a potential carrier system to deliver TAC. However, TAC + MAP conjugated even encapsulated in the NLC system demonstrated toxicity against the SH-SY5Y cell line.

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“…Commonly used solid lipids for NLC formulation are stearic acid, stearyl alcohol, glycerol monostearate, mono-stearin, etc., while common examples of liquid lipids involve the use of olive oil, sesame oil, almond oil, peanut oil, soyabean oil, oleic acid, corn oil, soy lecithin, phosphatidyl choline, vitamin E, etc. [69].…”

Section: Nanolipid Carriers (Nlcs) and Solid Lipid Nanoparticles (Slns)mentioning

confidence: 99%

Promising Nanotechnology Approaches in Treatment of Autoimmune Diseases of Central Nervous System

Demetzos

2020

Brain Sciences

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Multiple sclerosis (MS) is a chronic, autoimmune, neurodegenerative disease of the central nervous system (CNS) that yields to neuronal axon damage, demyelization, and paralysis. Although several drugs were designed for the treatment of MS, with some of them being approved in the last few decades, the complete remission and the treatment of progressive forms still remain a matter of debate and a medical challenge. Nanotechnology provides a variety of promising therapeutic tools that can be applied for the treatment of MS, overcoming the barriers and the limitations of the already existing immunosuppressive and biological therapies. In the present review, we explore literature case studies on the development of drug delivery nanosystems for the targeted delivery of MS drugs in the pathological tissues of the CNS, providing high bioavailability and enhanced therapeutic efficiency, as well as nanosystems for the delivery of agents to facilitate efficient remyelination. Moreover, we present examples of tolerance-inducing nanocarriers, being used as promising vaccines for antigen-specific immunotherapy of MS. We emphasize on liposomes, as well as lipid- and polymer-based nanoparticles. Finally, we highlight the future perspectives given by the nanotechnology field toward the improvement of the current treatment of MS and its animal model, experimental autoimmune encephalomyelitis (EAE).

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Recent strategies and advances in the fabrication of nano lipid carriers and their application towards brain targeting

Cited by 159 publications

References 296 publications

<p>Optimized Nanostructured Lipid Carriers Integrated into In Situ Nasal Gel for Enhancing Brain Delivery of Flibanserin</p>

<p>Optimized Nanostructured Lipid Carriers Integrated into In Situ Nasal Gel for Enhancing Brain Delivery of Flibanserin</p>

Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid Nanoparticles

Promising Nanotechnology Approaches in Treatment of Autoimmune Diseases of Central Nervous System

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