Nanoemulsion loaded with lycobetaine–oleic acid ionic complex: physicochemical characteristics, in vitro, in vivo evaluation, and antitumor activity

Neocryptolepine (5-methyl-5H-indolo[2,3-b] quinoline) analogs were synthesized and evaluated in vitro and in vivo for their effect versus Ehrlich ascites carcinoma (EAC). The analogs showed stronger cytotoxic activity against EAC cells than the reference drug. The in vivo evaluation of the target compounds against EAC-induced solid tumor in the female albino Swiss mice revealed a remarkable decrease in the tumor volume (TV) and hepatic lipid peroxidation. A noticeable increase of both superoxide dismutase (SOD) and catalase (CAT) levels was reported (p < 0.001), which set-forth proof of their antioxidant effect. In addition, the in vitro antioxidant activity of the neocryptolepine analogs was screened out using the DPPH method and showed promising activities activity. The histopathological investigations affirmed that the tested analogs have a remarkable curative effect on solid tumors with minimal side-effect on the liver. The study also includes illustrated mechanism of the antitumor activity at the cell level by flow cytometry. The cell cycle analysis showed that the neocryptolepine analogs extensively increase the aggregation of tumor cells in three phases of the cell cycle (G0/G1, S and G2/M) with the emergence of a hypo-diploid DNA content peak (sub-G1) in the cell cycle experiments, which is a clear-cut for the apoptotic cell population. Furthermore, the immunological study manifested a significant elevation in splenic lymphocyte count (p < 0.001) with the elevation of the responsiveness of lymphocytes to phytohemagglutinin (PHA). These results indicate that these naturally-based neocryptolepine alkaloids exhibit marked antitumor activity in vivo and represent an important lead in the development of natural-based anticancer drugs.

Download Full-text

EVALUASI IN VITRO-IN VIVO FILM TRANDERMAL DILTIAZEM HCL DENGAN PENINGKAT PENETRASI PEG 400 SEBAGAI ANTIHIPERTENSI

JIFFK : Jurnal Ilmu Farmasi dan Farmasi Klinik ◽

10.31942/jiffk.v16i01.2922 ◽

2019 ◽

Vol 16 (01) ◽

pp. 1

Author(s):

Yulias Ninik Windriyati ◽

Risha Fillah Fithria ◽

Fitria Dwi Kurniawati ◽

Ulfa Risalatul Mukaromah

Keyword(s):

Blood Pressure ◽

Physicochemical Characteristics ◽

Penetration Enhancer ◽

Transdermal Patch ◽

In Vivo Evaluation ◽

Peg 400 ◽

Transdermal Patches ◽

Diltiazem Hcl

ABSTRACTDiltiazem HCL is an antihypertensive that low oral bioavailability of 40%, so developed to transdermal preparations. A matrix type of transdermal patch of diltiazem HCl was prepared using polyvinyl alcohol and ethyl cellulose with PEG 400 as penetration enhancer. In vitro-in vivo evaluation were conducted to asses drug permeation through the skin and determine the effectiveness of transdermal film as an antihypertensive drug. Transdermal patches of diltiazem HCl were evaluated for physicochemical characteristics weight variation, thickness, folding endurance, moisture uptake, and drug content. In vitro permeation study was conducted using commercial semi permeable membrane in Franz diffusion cell. In vivo activity study was evaluated on male rat Wistar that induced NaCl with CODA non-invasive blood pressure method. Transdermal patches of diltiazem HCl were found no significant differences in terms of physicochemical characteristics. The in vitro skin permeation profiles showed increased flux values with the increase of PEG 400 as a penetration enhancer. The in vivo evaluation showed a reduction in systolic and diastolic blood pressure within one hour after the drug administration. Diltiazem HCl was able penetration into skin, absorbed in blood circulation and effective as antihypertensive via transdermal route.Keywords : antihypertension, diltiazem HCl, PEG 400, transdermal patch

Download Full-text