FORMULATION AND EVALUATION OF BILAYERED FELODIPINE TRANSDERMAL PATCHES: IN VITRO AND EX VIVO CHARACTERIZATION

Objective: Felodipine (FD) is an effective Biopharmaceutics Classification System Class II calcium channel blocker mainly used in the management of hypertension and angina pectoris. It has poor solubility and low oral bioavailability (15%). To overcome these disadvantages and to maintain constant plasma concentration for maximum therapeutic activity, there is a need to design an alternative route, that is, transdermal route. The pharmacokinetic parameters make FD a suitable candidate for transdermal delivery. The present investigation consists of the study of in vitro and ex vivo skin flux of FD from bilayered transdermal patches. Methods: The patches were fabricated by solvent casting method using hydrophilic and hydrophobic polymer with different composition. Tween 80 incorporated as solubilizer, polyethylene glycol 600 as plasticizer, menthol, eucalyptus oil, and lemongrass oil used as permeation enhancers, respectively. The prepared transdermal drug delivery system was extensively evaluated for in vitro release, ex vivo permeation through pig ear skin, moisture content, moisture absorption, water vapor transmission, and mechanical properties. The physicochemical interaction between FD and polymers was investigated by Fourier-transform infrared (FTIR) spectroscopy. Results: All the formulations exhibited satisfactory physicochemical and mechanical characteristics. A flux of 35.2 μg/cm2 h, 27.9 μg/cm2 h, and 25.25 μg/cm2 h was achieved for optimized formulations containing lemongrass oil, eucalyptus oil, and menthol, respectively, permeation enhances. Values of tensile strength (0.0652±0.034 kg/mm²) and elongation at break (0.8749±0.0.0029% mm²) revealed that formulation F9 was strong but not brittle. Drug and excipients compatibility studies showed no evidence of interaction between the active ingredient and polymers. Conclusion: Bilayered FD transdermal patches could be prepared with required flux and suitable mechanical properties

Pseudoanaeurysm of right uterine artery: Rare cause of secondary postpartum hemorrhage (PPH) & managed by uterine artery embolisation

A 24 yrs-old woman (G1P1) had an uneventful first pregnancy, delivered by emergency caesarian section at term. The patient was transferred to our institution on 24th postoperative day with symptoms of severe bleeding per vaginum with syncopal attacks of two episodes. On examination, her vitals were stable, the C- section scar was healthy and uterus well retracted and cervical OS closed with minimal bleeding. Her hemoglobin was 6.1gm/dl and 1 unit of compatible packed cell transfusion was given and broadspectrum antibiotics were started. Trans vaginal ultrasound scan (TVS) with color doppler was done. It confirmed postpartum uterus without any evidence of retained products of conception. Endometrial thickness was 7 mm. A hypoechoic lesion of size 1.7 x 1.0 cm with ‘yin and yang’ blood flow pattern was detected, posteroinferior to the site of scar in the lower segment, suggestive of pseudoaneurysm. CT angiography was done and it was confirmed as pseudoaneurysm of distal branches of right uterine artery. To preserve fertility, right uterine artery and pseudoaneurysm were selectively cannulated and embolization of pseudoaneurysm was performed using N-Butylcyano Acrylate with lipoidol mixture. A post embolization angiographic study was performed to ensure complete exclusion of aneurysm from circulation. She was asymptomatic on follow-up. Doppler and CT angiography are useful techniques to diagnose this condition. Being a minimally invasive procedure selective embolization should be done whenever feasible

<span style="font-size:11.0pt;font-family: "Times New Roman";mso-fareast-font-family:"Times New Roman";mso-bidi-font-family: Mangal;mso-ansi-language:EN-GB;mso-fareast-language:EN-US;mso-bidi-language: HI" lang="EN-GB">Evaluation of the anticancer potential of coffee<span style="font-size:11.0pt;font-family:"Times New Roman";mso-fareast-font-family: "Times New Roman";mso-bidi-font-family:Mangal;mso-ansi-language:EN-GB; mso-fareast-language:EN-IN;mso-bidi-language:HI" lang="EN-GB"> <span style="font-size:11.0pt;font-family:"Times New Roman";mso-fareast-font-family: "Times New Roman";mso-bidi-font-family:Mangal;mso-ansi-language:EN-GB; mso-fareast-language:EN-US;mso-bidi-language:HI" lang="EN-GB">beans: An <i style="mso-bidi-font-style: normal">in vitro</i> study</span></span></span>

266-271The aim of the present study was to evaluate the anticancer activity of the ethanol extract of raw coffee beans and identification of its active component. It was found that coffee bean ethanol extract, at concentration of 0.1µg/ml, has potent anti-proliferative effect against HeLa and PA-1 cell lines with decrease in percentage viability to less than 30% after 72 hrs of incubation. Partially purified green TLC fraction was also found to be cytotoxic to HeLa and PA-1 cell lines with reduction in percentage viability to 26.8 % and 13.6%, respectively, after 72 hrs of incubation. The extract and the fraction were able to induce apoptosis and nuclear fragmentation in the cells as evidenced by DNA fragmentation assay and fluorescence microscopy. Flow cytometry analyses confirmed the ability of the green fraction to arrest the cells at G0/G1- phase. Its non-cytotoxicity to human peripheral lymphocytes indicates its safety towards humans

In Vitro and In Vivo Demonstration of Human-Ovarian-Cancer Necrosis through a Water-Soluble and Near-Infrared-Absorbing Chlorin

With the objective of developing efficient sensitizers for therapeutic applications, we synthesized a water-soluble 5,10,15,20-tetrakis­(3,4-dihydroxyphenyl)­chlorin (TDC) and investigated its in vitro and in vivo biological efficacy, comparing it with the commercially available sensitizers. TDC showed high water solubility (6-fold) when compared with that of Foscan and exhibited excellent triplet-excited-state (84%) and singlet-oxygen (80%) yields. In vitro photobiological investigations in human-ovarian-cancer cell lines SKOV-3 showed high photocytotoxicity, negligible dark toxicity, rapid cellular uptake, and specific localization of TDC in neoplastic cells as assessed by flow-cytometric cell-cycle and propidium iodide staining analysis. The photodynamic effects of TDC include confirmed reactive-oxygen-species-induced mitochondrial damage leading to necrosis in SKOV-3 cell lines. The in vivo photodynamic activity in nude-mouse models demonstrated abrogation of tumor growth without any detectable pathology in the skin, liver, spleen, or kidney, thereby demonstrating TDC application as an efficient and safe photosensitizer