Cancer is one of the most leading causes of death in the world. Ovarian cancer is the seventh most common cancer in women. Also, it has the highest, mortality rate among female reproductive system cancers (1). According to the American Cancer Society in 2018, 22240 new cases of ovarian cancer will be diagnosed and 14070 women will die of ovarian cancer in the United States (2). The highest incidences are related in Europe, Canada and the United States. The lowest incidences are reported in China and Africa. According to GLOBOCAN 2008 database, the incidence rates are reported as over 11 cases per 100000 in Europe, less than 3 cases per 100000 in Africa and 4-8 cases per 100000 in South American, Asian and Caribbean countries (3). The latest cancer mortality statistics of the World Health Organization (WHO) showed that mortality will increase by approximately 45% until 2030 (4). Ovarian cancer has different risk factors like family history, age, early age menarche, menopause, parity, oral contraceptive use, lactation, obesity, cigarette smoking and alcohol consumption (5-7). Epithelial ovarian cancer is the most common type of ovarian cancer. Early diagnosis increases the chances successful treatment. The pathogenesis of ovarian cancer hasnít been elucidated yet, but ovulation, hormonal factors and inflammations have an important role in it (8, 9). There are two types of ovarian tumors. Type I tumors tend to be less aggressive and slow-growing like low grade malign serous tumors, low grade malign endometrioid carcinoma and mucinous carcinoma. Type II tumors are more aggressive than Type I tumors. They are high grade malign serous carcinoma, carcinosarcoma and undifferentiated carcinoma (10, 11). Ovarian cancer is staged by using the FIGO staging system which has 4 stages. A tumor is limited to the ovary at stage I. During stage II, tumor involves one or both of the ovaries. Pelvic extension and primary peritoneal tumor occurred. At stage III,
The main purpose of this study was to prepare Azithromycin (AZM) loaded Eudragit RL 100 (ERL) nanoparticles in order to increase the antibacterial activity of AZM and to compare the drug release profiles of the formulations at the stomach and intestinal pH. AZM-NP-1:5 (AZM:ERL = 1:5) and AZM-NP-1:10 (AZM:ERL = 1:10) nanoparticles were prepared using different drug-polymer ratios. Particle size and zeta potential were analysed and physicochemical characterization was performed using Scanning Electron Microscope (SEM), Fourier Transform Infrared (FT-IR) Spectroscopy, Proton Nuclear Magnetic Resonance ( 1 H-NMR) Spectroscopy, Differential Scanning Calorimetry (DSC) and X-ray Diffraction (XRD). AZM-NP-1:10 have 554.4 ± 29.3 nm size, + 15.4 ± 3.18 mV charge with 77.06 ± 3.63% DL%. In the in vitro release tests, after the first 3 hours, 49.35 ± 1.64% of the active ingredient was released from AZM-NP-1:10 at pH 1.2 HCl medium and the release was found to fit Korsmeyer-Peppas kinetic model. A similar release profile (f2 = 71) of 51.40 ± 1.71% for the first 3 hours was also obtained for AZM-NP-1:10 in PBS at pH 6.8. The Minimum Inhibitory Concentration (MIC) of free AZM and AZM-NP-1:10 against Staphylococcus aureus was found to be 2 and 0.5 µg/mL, respectively. The activity of AZM started to decrease after 6 hours while AZM-NP-1:10 presented a continuous antibacterial activity for 24 hours. AZM-NP-1:10 exhibited an enhanced antibacterial activity and a prolonged drug release pattern compared to free AZM, allowing for more effective treatment with fewer side effects. RezumatScopul principal al acestui studiu a fost de a prepara nanoparticule încărcate cu azitromicină (AZM) și Eudragit RL 100 (ERL), pentru a crește activitatea antibacteriană a AZM și pentru a compara profilurile de eliberare ale formulărilor la pH gastric și intestinal. Nanoparticulele AZM-NP-1:5 (AZM:ERL = 1:5) și AZM-NP-1:10 (AZM:ERL = 1:10) au fost preparate folosind diferite rapoarte medicament-polimer. Dimensiunea particulelor și potențialul zeta au fost analizate și caracterizarea fizicochimică a fost efectuată folosind microscopul electronic cu scanare (SEM), spectroscopie în infraroșu cu transformată Fourier (FT-IR), spectroscopie de rezonanță magnetică nucleară cu protoni ( 1 H-NMR), calorimetrie cu scanare diferențială (DSC) și difracția de raze X (XRD).
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