A Nasal Temperature and pH Dual-Responsive In Situ Gel Delivery System Based on Microemulsion of Huperzine A: Formulation, Evaluation, and In Vivo Pharmacokinetic Study

Chen, Yifan; Cheng, Gang; Hu, Rongfeng; Chen, Shengqi; Lu, Wenjie; Gao, Song; Xia, Hongmei; Wang, Bin; Sun, Chuan-bin; Nie, Xiangjiang; Shen, Qiang; Fang, Wenyou

doi:10.1208/s12249-019-1513-x

Cited by 28 publications

(20 citation statements)

References 47 publications

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“…The most frequently used synthetic monomer with acidic characteristics are acrylic acid, methacrylic acid, maleic anhydride, N,N-dimethylaminoethyl methacrylate and sulphonamide-containing polymers [2,18,20,91,109]. Weak synthetic polybases, such as aromatics 4-vinylpyridine, 2-vinylpyridine, poly(vinyl imidazole), poly(N,N-dimethyl aminoethyl methacrylate), and poly(N,N-diethyl aminoethyl methacrylate), accept protons at low pH [50,110,111]. There is also a large group of natural polymers used in pH-responsive HGs that has advantages over synthetic polymers due to their degradability within the human body, making them excellent biocompatible components in drug delivery [9,33,88,112].…”

Section: Ph- Electric-and Magnetic-responsive Hydrogelsmentioning

confidence: 99%

“…Suitable controlled-release mechanisms include (Figure 8): diffusion [17], swelling [68], chemical and environmental stimuli (degradation or deformation) [67]. Drug release from HGs in response to environmental stimuli may occur due to changes in pH [110,204], temperature [110,[205][206][207], electric field [109,111,208] or ionic strength [209,210]. Some ideas are schematically presented in Figure 8 [17].…”

Section: Release Mechanism Of Drug From Hydrogel Matricesmentioning

confidence: 99%

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Hydrogels as Potential Nano-, Micro- and Macro-Scale Systems for Controlled Drug Delivery

2020

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This review is an extensive evaluation and essential analysis of the design and formation of hydrogels (HGs) for drug delivery. We review the fundamental principles of HGs (their chemical structures, physicochemical properties, synthesis routes, different types, etc.) that influence their biological properties and medical and pharmaceutical applications. Strategies for fabricating HGs with different diameters (macro, micro, and nano) are also presented. The size of biocompatible HG materials determines their potential uses in medicine as drug carriers. Additionally, novel drug delivery methods for enhancing treatment are discussed. A critical review is performed based on the latest literature reports.

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Section: Ph- Electric-and Magnetic-responsive Hydrogelsmentioning

confidence: 99%

Section: Release Mechanism Of Drug From Hydrogel Matricesmentioning

confidence: 99%

Hydrogels as Potential Nano-, Micro- and Macro-Scale Systems for Controlled Drug Delivery

2020

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“…In rats, HupA injected intraperitoneally (ip) showed the same efficacy of AChE inhibition as displayed following oral administration, althoughip administration of tacrine and donepezil showed higher inhibition on both AChE activity and serum BuChE. 22 The inhibitory action of HupA on brain AChE was not as much as that of donepezil after the intraventricular injection, but more efficient than tacrine. 23 Maximal AChE inhibition in rat cortex and whole brain was reached at 30-60 min and maintained for 360 min following oral administration of 0.36 mg/kg HupA.…”

Section: In Vitro Studies On Huperzinementioning

confidence: 93%

Huperzinea: Pharmacological and Therapeutic Potential

Dubey¹,

Ahmad²,

Sharma³

et al. 2020

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Introduction: Huperzine A (HupA) is derived from a club moss (Huperzia serrata). It is a potent and reversible inhibitor of acetyl cholinesterase (AChE). Chemically, it is a sesquiterpene alkaloid. It has been used for the treatment of swelling, fever and blood disorders for centuries in China. Methodology: The literature available on Huperzine was thoroughly studied. It has shown much beneficial effect since ages. It is a established Nootropic agent and widely used in the treatment of Alzheimer's disease. The plant has shown promising results in vivo and in vitro studies. Results and Conclusion: The present review highlights the pharmacological potential of Huperzine with its pharmacokinetic and pharmacokinetic studies and it's rational for future prospective.

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“…Considering that the pH range of nasal mucosa is between 5 and 6.5 [ 10 ], to avoid nasal irritation and local toxicity, after self-emulsification, the pH of the formed emulsions should be within this interval. Of the studies revised here that developed SEDDS for nose-to-brain targeting, only Meirinho et al [ 28 ], Chen et al [ 30 ], and Nagaraja et al [ 5 ] investigated the final pH of, respectively, SMEDDS loaded with perampanel, the temperature and pH-responsive in situ gel containing SMEDDS loaded with huperzine A, and naringin in situ gelling SNEDDS, being all within acceptable values ( Table 1 ). The morphology and percentage of transmittance can also be examined to explore the shape and the clearness of SEDDS after suitable dilutions [ 7 , 8 ].…”

Section: Sedds Development For Delivery Of Neurotherapeutics Agents T...mentioning

confidence: 96%

Self-Emulsifying Drug Delivery Systems: An Alternative Approach to Improve Brain Bioavailability of Poorly Water-Soluble Drugs through Intranasal Administration

2022

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Efforts in discovering new and effective neurotherapeutics are made daily, although most fail to reach clinical trials. The main reason is their poor bioavailability, related to poor aqueous solubility, limited permeability through biological membranes, and the hepatic first-pass metabolism. Nevertheless, crossing the blood–brain barrier is the major drawback associated with brain drug delivery. To overcome it, intranasal administration has become more attractive, in some cases even surpassing the oral route. The unique anatomical features of the nasal cavity allow partial direct drug delivery to the brain, circumventing the blood–brain barrier. Systemic absorption through the nasal cavity also avoids the hepatic first-pass metabolism, increasing the systemic bioavailability of highly metabolized entities. Nevertheless, most neurotherapeutics present physicochemical characteristics that require them to be formulated in lipidic nanosystems as self-emulsifying drug delivery systems (SEDDS). These are isotropic mixtures of oils, surfactants, and co-surfactants that, after aqueous dilution, generate micro or nanoemulsions loading high concentrations of lipophilic drugs. SEDDS should overcome drug precipitation in absorption sites, increase their permeation through absorptive membranes, and enhance the stability of labile drugs against enzymatic activity. Thus, combining the advantages of SEDDS and those of the intranasal route for brain delivery, an increase in drugs’ brain targeting and bioavailability could be expected. This review deeply characterizes SEDDS as a lipidic nanosystem, gathering important information regarding the mechanisms associated with the intranasal delivery of drugs loaded in SEDDS. In the end, in vivo results after SEDDS intranasal or oral administration are discussed, globally revealing their efficacy in comparison with common solutions or suspensions.

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A Nasal Temperature and pH Dual-Responsive In Situ Gel Delivery System Based on Microemulsion of Huperzine A: Formulation, Evaluation, and In Vivo Pharmacokinetic Study

Cited by 28 publications

References 47 publications

Hydrogels as Potential Nano-, Micro- and Macro-Scale Systems for Controlled Drug Delivery

Hydrogels as Potential Nano-, Micro- and Macro-Scale Systems for Controlled Drug Delivery

Huperzinea: Pharmacological and Therapeutic Potential

Self-Emulsifying Drug Delivery Systems: An Alternative Approach to Improve Brain Bioavailability of Poorly Water-Soluble Drugs through Intranasal Administration

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