Abstract
Objective: Successful treatment of glioma still remains a tough challenge. The present study aims at the development and evaluation of carmustine loaded nanosize phospholipid vesicles (CNLVs) for the treatment of glioma.
 Methods: The experimental NLVs were developed by conventional lipid layer hydration technique and were characterized by different in vitro tools such as diffraction light scattering (DLS), zeta potential, field emission scanning electron microscopy (FESEM), cryo-transmission electron microscopy (cryo-TEM), in vitro drug loading capacity, drug release study etc. In vitro cytotoxicity and cellular uptake of the optimized drug-loaded NLVs were carried out in U87MG human glioblastoma cell line. In vivo pharmacokinetic study was conducted in Swiss albino mice.
 Results: DLS data showed an average vesicle diameter of 92 nm with narrow size distribution. Optimized CNLVs were spherical in shape with a smooth surface as depicted from FESEM data. Cryo-TEM study confirmed formation of unilamellar vesicles with intact outer bilayer. A reasonable drug loading of 7.8 % was reported for the optimized CNLVs along with a sustained release of CS over a 48 h study period. In vitro cytotoxicity assay revealed a considerable higher toxicity of CNLVs than free drugs in the U87MG cells. Confocal microscopy showed a satisfactory internalization of the optimized drug-loaded NLVs in the tested cell line. Pharmacokinetic data demonstrated an enhanced mean residence time of optimized CNLVs in blood than free drug.
 Conclusion: Results depicted the potential of experimental CNLVs for the treatment of glioma after further in vivo tests.
Highlights
Successful treatment of brain tumor still remains a herculean task for medical experts
According to a report from the American Cancer Society, an estimated 23,890 adults in the United States have been diagnosed with primary brain tumor in the year 2019-20, along with about 3,540 children under the age of 15, which exposes the inefficiency of the present therapy [2]
In the lieu of this, the present study aims to investigate the anticancer potential of phospholipid based nanovesicular carrier systems loaded with CS for glioma therapy
Summary
Successful treatment of brain tumor still remains a herculean task for medical experts. Glioma is the most common type of primary brain tumor that develops in the glial cells of the brain [1]. Based on the type of glial cells, gliomas can be of astrocytomas, ependymomas, oligodendrogliomas etc. Many conventional chemotherapeutics drugs are though available in the market, but the majority of them fails to maintain the desired therapeutic concentration in the brain tissue due to their inability to pass effectively through BBB [4]. Severe doserelated toxic effects associated with conventional chemotherapy throw further challenges for the successful treatment of glioma. Among various types of nanocarrier platforms, nanosize lipid based vesicular carriers (NLVs) have been largely preferred for the successful delivery of toxic chemotherapeutic drugs to the brain [8]. Due to high lipophilic nature as well as ultra-small size, they fulfill the prime requisite criteria to overcome BBB to get into the brain
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