Surface functionalized folate targeted oleuropein nano-liposomes for prostate tumor targeting: Invitro and invivo activity.

AIMS: This study aims to develop and evaluate oleuropein loaded surface functionalized folate-targeted - PEG liposomes for the effective management of prostate cancer in an animal model. MATERIALS AND METHODS: Film hydration-cum-extrusion technique was used to produce liposomes. Particle size, entrapment efficiency, drug loading, electron microscopy, and drug release study were performed for the characterization. Cell viability and various in vitro studies (phosphatidylserine internalization, TUNEL assay, measurement of mitochondrial membrane potential and caspase-3 assay) were performed to compare the anticancer and apoptotic effects of developed liposomes against the plain oleuropein. Comparative pharmacokinetic profiling and anticancer efficacy studies including a change in tumor volume, body weight, and survival analysis were performed in mice model. KEY FINDINGS: The developed liposomes (OL-FML) showed the particle size of 184.2 ±â€¯9.16 nm, the zeta potential of 1.41 ±â€¯0.24 mV, entrapment efficiency of 63.52 ±â€¯4.15% and drug loading of 21.31 ±â€¯2.37%. OL-FML showed higher in vitro anti-proliferative effect and apoptosis on 22Rv1 cells. In vivo pharmacokinetic study revealed a nearly 6 fold increase in the bioavailability of OL-FML (AUC0→∞ = 641.78 ±â€¯103.764 µg/mL·hr) as compared to OL solution (AUC0→∞ = 104.11 ±â€¯18.374 µg/mL·hr) in mice. Increased tumor suppression, weight loss resistance, and survival probability were observed in 22Rv1 induced tumor-bearing mice with OL-FML treatment as compared to OL. SIGNIFICANCE: The study provides conclusive evidence for the utilization of combining passive and active targeting strategy to enhance the anticancer effect of OL.

Antimicrobial sensitivity pattern of bacterial pathogens in urinary tract infections in South Delhi, India.

Seventy-four bacterial proven cases of urinary tract infections were studied, and identified by Mac Conkey agar and blood agar medium separately; all the isolates were subjected to antimicrobial sensitivity testing by Stokes technique. Ninty-six percent of total isolated organisms were found to be gram negative while remaining 4% were gram positive. Among gram negatives, E. coli and gram positive S. aureus were the most prevalent organisms. The percentage of gram negative isolates were as follows, E. coli (79.7%) followed by Klebsiella (9.5%), Pseudomonas, Acinetobacter were (2.7% each), Proteus constituted (1.4%). and among gram positive S. aureus (4%). The antibiotic resistance of identified organisms was carried out by disc-diffusion method with commercially available disc of thirteen antibiotics having different mode of actions such as inhibition of cell wall synthesis, membrane permeability alternatives, inhibition of protein synthesis and DNA synthesis inhibitors. Gram negatives showed more resistance to these antibiotics as compared to gram positive organisms. The most effective antibiotic for gram negative UTI isolates is amikacin showing 63% efficacy followed by Cefotaxime 55% efficacy, Amoxicillin and Ciprofloxacin with (49% each) efficacy. Among gram positives, Chloramphenicol, Co-trimoxazole, Gentamicin, Amikacin, Ciprofloxacin and Cefotaxime are most effective with (66.6% each) efficacy, then Ampicillin, Amoxicillin, Tetracycline and norfloxacin with (33.3% each) efficacy.

Feasibility of Assam Bora rice starch as a compression coat of 5-fluorouracil core tablet for colorectal cancer.

The colon and rectum are the parts of digestive system of human beings. Cancer affecting either of these organs may be called colorectal cancers. Conventional cancer chemotherapy is not very effective for treatment of colorectal cancer, as the drug molecule does not reach the target site at therapeutic concentration, on the other side they produces sever systemic toxic effect. Aim of this study was to develop a novel colon targeted Assam Bora rice starch compression coated tablet for site specific delivery of 5-FU to the colon without the drug being released in stomach or small intestine. Core tablet of 5-FU was prepared using microcrystalline cellulose (MCC) and spray dried lactose by direct compression method. The in vitro drug release study in different physiological environment confirmed insignificant release of 5-FU in physiological condition of stomach and small intestine further fast and major drug release in caecal content. In vivo drug absorption of optimized formulation was performed in order to establish its targeting potential in colon. It is concluded from the present study that Assam Bora rice starch can be used as a drug carrier for an effective colon targeted delivery system for drugs effective against the large intestine resident disease condition.