Poly lactic acid is a biodegradable, biocompatible, and non-toxic polymer, widely used in many pharmaceutical preparations such as controlled release formulations, parenteral preparations, surgical treatment applications, and tissue engineering. In this study, we prepared lipid-polymer hybrid nanoparticles for topical and site targeting delivery of Norfloxacin by emulsification solvent evaporation method (ESE). The design of experiment (DOE) was done by using software to optimize the result, and then a surface plot was generated to compare with the practical results. The surface morphology, particle size, zeta potential and composition of the lipid-polymer hybrid nanoparticles were characterized by SEM, TEM, AFM, and FTIR. The thermal behavior of the lipid-polymer hybrid nanoparticles was characterized by DSC and TGA. The prepared lipid-polymer hybrid nanoparticles of Norfloxacin exhibited an average particle size from 178.6 ± 3.7 nm to 220.8 ± 2.3 nm, and showed very narrow distribution with polydispersity index ranging from 0.206 ± 0.36 to 0.383 ± 0.66. The surface charge on the lipid-polymer hybrid nanoparticles were confirmed by zeta potential, showed the value from +23.4 ± 1.5 mV to +41.5 ± 3.4 mV. An Antimicrobial study was done against Staphylococcus aureus and Pseudomonas aeruginosa, and the lipid-polymer hybrid nanoparticles showed potential activity against these two. Lipid-polymer hybrid nanoparticles of Norfloxacin showed the %cumulative drug release of 89.72% in 24 h. A stability study of the optimized formulation showed the suitable condition for the storage of lipid-polymer hybrid nanoparticles was at 4 ± 2 °C/60 ± 5% RH. These results illustrated high potential of lipid-polymer hybrid nanoparticles Norfloxacin for usage as a topical antibiotic drug carriers.
Background
Ethosomes have been widely used in Transdermal Drug Delivery System (TDDS) as they increase the permeation of drug across the skin.
Methods
Flurbiprofen loaded vesicular ethosomes were formulated, optimized and characterized for particle size, entrapment efficiency, poly dispersive index (PDI), microscopy using Atomic force microscopy (AFM), Scanning electron microscope (SEM) and Transmission electron microscopy (TEM) and Interaction of drug and excipients were studied using Fourier transform infra-red (FTIR) spectroscopy, Differential scanning colorimetry (DSC), Thermo gravimetric analysis (TGA). Further, ethosomal formulations of flurbiprofen were evaluated for stability study of three months and in vitro drug permeation study was carried out using albino rat skin. In addition, skin irritation test was evaluated by Draize test and in vivo study of prepared formulation was examined through paw edema assay by inducing carrageenan and cold plate method.
Results
Amongst all formulations, EF5 formulation exhibited ideal surface morphology, with maximum entrapment efficiency (95%) with optimal excipient concentration i.e. 200 mg phospholipid and 35% ethanol. The ideal vesicle size was achieved as 162.2 ± 2 nm, with zeta potential − 48.14 ± 1.4 mV with the PDI of 0.341. In-vitro permeation study shows a release of 82.56 ± 2.11 g/cm
2
in 24 h and transdermal flux was found as 226.1 μg/cm
2
/h. Cold plate test indicates that the formulation EF5 showed a marked analgesic activity and Carrageenan induced paw edema test indicates that the formulation EF5 inhibits the increase in paw edema. Ethosomal suspension at 4 °C showed maximum stability.
Conclusions
The overall study concluded that this ethosomal approach offers a new delivery system for sustained and targeted delivery for flurbiprofen.
Electronic supplementary material
The online version of this article (10.1186/s12944-019-1064-x) contains supplementary material, which is available to authorized users.
The main purpose of the present study was to synthesize graphene quantum dots (GQDs)from the flowers of Clitoria ternatea with the help of one-pot microwave-assisted green synthesis for the treatment of Alzheimer's disease. Further, the synthesized graphene quantum dots show a particle size of 10 nm ±1.3, a PDI of 0.354 ± 1.8, and a ζ potential of −46 ± 0.4, indicating the good stability of the quantum dots. With the help of scanning electron microscopy (SEM) and transfer electron microscopy (TEM) examination, the surface microscopic behavior of the synthesized quantum dots was determined. The presence of functional groups in the quantum dots was determined by Fouriertransform infrared spectroscopy (FTIR) study, the chemical state information on the sample was determined with the help of X-ray photoelectron spectroscopy (XPS), and the surface area of the dots was determined with the help of a surface area analyzer. With the help of a radial arm maze and water morris maze assay, the learning and memory capacity of the quantum dots was assessed, and the results show that the ctGQDs significantly decreased the transfer latency to reach the baited arm in 10.37 ± 1.65 s or to the hidden platform in 18.42 ± 0.99 s in 7 days. The synthesized quantum dots show more inhibition of the acetyl cholinesterase enzyme, i.e., 86.32 ± 1.52%, as compared to that of pure donepezil, i.e., 72.46 ± 2.21%. ctGQDs considerably increased the level of glutathione and protein and decreased the level of lipid peroxide and nitric oxide. The histopathological image of ctGQDs shows more preservation of small pyramidal cell and treats the disorganization of the cells. These results suggest that the quantum dots significantly crossed the blood−brain barrier since they were small in size and were effective in reducing Alzheimer-like symptoms in rodents, and thus, it can be concluded that Clitoria ternatea flowers can be used as an adjuvant in the treatment of Alzheimer's.
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