Abstract
The aim of this study was to develop topical self-microemulsifying drug delivery systems (SMEDDS) containing antitumor agents (bleomycin, cisplatin and ifosfamide) and to investigate their inhibitory potential in SMEDDS on human cervical cancer HeLa cells. The physicochemical properties of cytostatic drug loaded SMEDDS were characterized. The cytotoxicity of main components of SMEDDS was also investigated. Their IC50 values were determined. HeLa cells were treated by different concentrations of cisplatin, bleomycin and ifosfamide alone and in various SMEDDS. The inhibitory effect on cell growth was analyzed by MTT cell viability assay. Inflammation is a driving force that accelerates cancer development. The inhibitory effect of these antitumor agents has also been tested on HeLa cells in the presence of inflammatory mediators (IL-1-β, TNF-α) as an in vitro model of inflamed human cervix. Significant differences in the cytotoxicity of cytostatic drugs alone and in SMEDDS have been found in a concentration-dependent manner. The self-micro emulsifying system may potentiate the effectiveness of bleomycin, cisplatin and ifosfamide topically. The effect of SMEDDS containing antitumor agents was decreased significantly in the presence of inflammatory mediators. According to our experiments, the optimal SMEDDS formulation is 1:1:2:6:2 ratios of Isopropyl myristate, Capryol 90, Kolliphor RH 40, Cremophor RH40, Transcutol HP and Labrasol. It can be concluded that SMEDDS may increase the inhibitory effect of bleomycin, ifosfamide and cisplatin on human cervical cancer HeLa cells. Inflammation on HeLa cells hinders the effectiveness of SMEDDS containing antitumor agents. Our results might ensure useful data for development of optimal antitumor formulations.
Highlights
Uterine and cervix carcinoma is the first cause of gynecological cancer mortality in developing countries [1]
The IC50 concentrations of cisplatin, blemycin and ifosfamide was mixed and incorporated in the compositions. (Table 2.) We found that the inhibitory effect of BIP combination was higher than the applied antitumor agents alone
The inhibitory effect of six different self-microemulsifying drug delivery systems (SMEDDS) compositions containing cisplatin, bleomycin sulfate, ifosfamide and their mixture was investigated on human cervical cancer HeLa cells
Summary
Uterine and cervix carcinoma is the first cause of gynecological cancer mortality in developing countries [1]. Cervical cancer is well-known to be a chronic inflammatory disease of multifactorial etiology [2]. Antitumor agents have played an important role in cervical cancer therapy [3]. Cisplatin is one of the main selected antitumor agents, but the remission rate of cervical cancer in advanced stage by cisplatin alone is only 17%–21% [4]. Cisplatin, bleomycin and ifosfamide (BIP) in combination has been applied against inoperable cervical cancer [5]. Many active pharmaceutical ingredients (API) have been developed to improve the efficacy of chemotherapy [6,7]
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