Preparation and characterization of memantine loaded polycaprolactone nanocapsules for Alzheimer’s disease

Mahmoudi, Masomeh; Saeidian, Hamid; Mirjafary, Zohreh; Mokhtari, Javad

doi:10.1007/s10934-020-00981-2

Cited by 14 publications

(6 citation statements)

References 32 publications

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“…The presence of the ionized carboxylic groups of PCL was the cause of the negative zeta potentials observed for MPs. 42 The amount of MPs adhering to the bacterial cell surface of SA corresponds closely with the values of zeta potential difference. 43 It has been previously reported that the zeta potential value of SA was −35.6 mV.…”

Section: Physicochemical Characterization Of Optimized Mp Chl−pcl For...supporting

confidence: 55%

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Enhancement in Site-Specific Delivery of Chloramphenicol Using Bacterially Sensitive Microparticle Loaded Into Dissolving Microneedle: Potential For Enhanced Effectiveness Treatment of Cellulitis

Mudjahid

Nainu

Utami

et al. 2022

ACS Appl. Mater. Interfaces

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One of the biggest challenges in infectious disease treatment is the existence of bacterial infections in underskin wound tissue, such as cellulitis. Compared to other treatments, it is harder for antibacterial drugs to penetrate the physical barrier on the affected skin with a nonspecific target, making conventional therapy for cellulitis infection more difficult and considered. In this novel research, we pioneer a combined strategy of dissolving microneedles (MNs) and bacteria-sensitive microparticles (MPs) for enhanced penetration and targeted delivery of chloramphenicol (CHL) to the infection site specifically. The polycaprolactone polymer was used to make MPs because of its sensitivity to bacterial enzyme stimuli. The best microparticle formulation was discovered and optimized using the Design–Expert application. Furthermore, this study evaluated the antibacterial activity of MPs in vitro and in vivo on the mutant Drosophila larval infection model. This strategy shows improvement in the antibacterial activity of MPs and higher retention duration compared to conventional cream formulation, and the inclusion of these MPs into dissolving MNs was able to greatly improve the dermatokinetic characteristics of CHL in ex vivo evaluation. Importantly, the antimicrobial efficacy in an ex vivo infection model demonstrated that, following the use of this strategy, bacterial bioburdens decreased by up to 99.99% after 24 h. The findings offered a proof of concept for the enhancement of CHL dermatokinetic profiles and antimicrobial activities after its preparation into bacteria-sensitive MPs and distribution by MNs. Future research should investigate in vivo effectiveness in an appropriate animal model.

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Section: Physicochemical Characterization Of Optimized Mp Chl−pcl For...supporting

confidence: 55%

“…The zeta potential measurement for microparticles (MPs) was −7.54 ± 0.65 mV. The presence of the ionized carboxylic group s of PCL was the cause of the negative zeta potentials observed for MPs . The amount of MPs adhering to the bacterial cell surface of SA corresponds closely with the values of zeta potential difference .…”

Section: Resultsmentioning

confidence: 75%

Enhancement in Site-Specific Delivery of Chloramphenicol Using Bacterially Sensitive Microparticle Loaded Into Dissolving Microneedle: Potential For Enhanced Effectiveness Treatment of Cellulitis

Mudjahid

Nainu

Utami

et al. 2022

ACS Appl. Mater. Interfaces

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“…Assuming a spherical and fcc shaped nanosphere, the average number of gold atoms (N) per nanosphere was calculated using Eq. ( 1) [32], where π is the circumference of a sphere (3.14), ρ is the density for fcc gold ( 19.3g/cm 3 ), N A is Avogadro's number (the number of atoms per mole) ( 6.02310 23 ), M is the atomic weight of gold (197 g/mol), and D is the average core diameter of nanospheres that summarized in Table 2.…”

Section: Gold Nanospheres' Concentration and Extinction Coefficientmentioning

confidence: 99%

“…Memantine prefers to interact with cation channels controlled by the N-methyl-D-aspartate (NMDA) receptor. Despite these antagonistic effects, memantine has not been shown to stop or slow the neurodegeneration seen in people with Alzheimer’s disease [ 23 , 24 ]. Nano-delivery of memantine using AuNSs may improve its pharmacological effect.…”

Section: Introductionmentioning

confidence: 99%

Hydrophilic gold nanospheres: influence of alendronate, memantine, and tobramycin on morphostructural features

et al. 2022

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Turkevich gold nanospheres are the original nanospheres that have been modified over time. Its combination with targeting medications such as alendronate, memantine, and tobramycin will provide additional benefits in targeting specific areas in the bone, brain, and microorganisms, respectively. Hence, The reactivity and stability of nanospheres with various drug concentrations (milli-,micro-, and nano-levels) have been studied. With alendronate, the absorbance spectra of nanospheres at $$\uplambda _{max}$$ λ max 520 nm were always stable and no redshifts occurred. In contrast, the spectra with memantine and tobramycin were stable at the nano-level and redshifts occurred at the milli- and micro-levels. HRTEM and DLS revealed that the core diameter was relatively stable in all cases, whereas the hydrodynamic diameter and zeta potential varied with varying drug concentrations. Increasing concentration increased hydrodynamic diameter slightly with memantine (from 64.99 to 98.41 nm), dramatically with tobramycin (from 135.3 to 332.16 nm), and almost negligibly with alendronate (from 52.08 to 58.94 nm ). Zeta Potential, conversely, is reduced as concentration increases. Memantine had the greatest reduction in negativity, followed by tobramycin, but alendronate had a slight increase in negativity. Benefits from this research would be in targeted drug delivery, where stability and reactivity of gold nanospheres are critical.

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“…However, this drug has a short biological half-life of 2-3 h, and its high doses are associated with gastrointestinal, cholinergic and hepatic side effects. Given the experience of the present research group related to the use of PCL nanocapsules in the pharmaceutical and agricultural industries [41][42][43], in the present study, it has been attempted to load 7-MEOTA drug on PCL nanoparticles as a useful release system and investigate its physico-chemical properties using various analytical techniques.…”

Section: Introductionmentioning

confidence: 99%

Controlled Release 7-Methoxytacrine-Polycaprolactone Nanocapsules Drug-Delivery System for Alzheimer's Disease Treatment: Synthesis and Physico-Chemical Characterization

et al. 2021

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Alzheimer's disease is the most prevalent cause of dementia in aging people. 7-Methoxytacrine (7-MEOTA) is one of the approved drugs for the treatment of this disease. In the current study, a 7-MEOTA delivery system has been prepared based on the polycaprolactone nanocapsules (7-MEOTA@PCL) and its physico-chemical properties were investigated as well. The drug amount loaded in nanocapsules has been estimated 65%. The average particle size of the 7-MEOTA@PCL nanocapsules was around 237 nm with polydispersity index of 0.31 and negative surface charge (-21.2 mV). The prepared nanoparticles are stable upon 40 days storage at 25 °C, without any decomposition. The morphological analysis of the 7-MEOTA@PCL nanoparticles indicated that the nanoparticles are spherical, and free of any aggregation. In vitro release experiments revealed controlled release of the 7-MEOTA from the polycaprolactone nanocapsules. Application of the Korsmeyer-Peppas model to the release kinetics data showed that the release of the drug was by diffusion Fick's law.

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Preparation and characterization of memantine loaded polycaprolactone nanocapsules for Alzheimer’s disease

Cited by 14 publications

References 32 publications

Enhancement in Site-Specific Delivery of Chloramphenicol Using Bacterially Sensitive Microparticle Loaded Into Dissolving Microneedle: Potential For Enhanced Effectiveness Treatment of Cellulitis

Enhancement in Site-Specific Delivery of Chloramphenicol Using Bacterially Sensitive Microparticle Loaded Into Dissolving Microneedle: Potential For Enhanced Effectiveness Treatment of Cellulitis

Hydrophilic gold nanospheres: influence of alendronate, memantine, and tobramycin on morphostructural features

Controlled Release 7-Methoxytacrine-Polycaprolactone Nanocapsules Drug-Delivery System for Alzheimer's Disease Treatment: Synthesis and Physico-Chemical Characterization

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