Passive Vectoring of a Colloidal Carrier System for Sodium Stibogluconate: Preparation, Characterization and Performance Evaluation

Karajgi, Jayant; Jain, Nishi; Vyas, Suresh P.

doi:10.3109/10611869308996077

Cited by 11 publications

(4 citation statements)

References 19 publications

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“…The mean size of a colloidal drug carrier is an important requisite that can influence the delivery device's biological effectiveness (26,42). In order to obtain liposome colloidal suspensions with a reduced mean size, the extrusion through polycarbonate filters was carried out.…”

Section: Resultsmentioning

confidence: 99%

Ofloxacin-Loaded Liposomes: In Vitro Activity and Drug Accumulation in Bacteria

Furneri¹,

Fresta

Puglisi

et al. 2000

Antimicrob Agents Chemother

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Different ofloxacin-loaded unilamellar vesicles were prepared by the extrusion technique, and their antimicrobial activities were determined in comparison to those of the free drug by means of MIC determinations with both American Type Culture Collection standards and wild-type bacterial strains (six strains of Enterococcus faecalis, seven strains of Escherichia coli, six strains of Staphylococcus aureus, and six strains of Pseudomonas aeruginosa). The accumulation of ofloxacin and liposome-ofloxacin was measured by determining the amount of the drug inside the bacteria as a function of time. Encapsulated fluoroquinolone yielded MICs which were at least twofold lower than those obtained with the free drug. In particular, liposomes made up of dimyristoylphosphatidylcholine-cholesterol-dipalmitoylphosphatidylserine and dimyristoylphosphatidylcholine-cholesterol-dihexadecylphosphate (4:3:4 molar ratio) provided the best improvement in antimicrobial activity against the various bacterial strains investigated. The liposome formulation produced higher intracellular fluoroquinolone concentrations than those achieved simultaneously with the free drug in both E. coli and P. aeruginosa.Since the discovery of the original DNA gyrase inhibitor nalidixic acid, numerous structural modifications have been carried out to the quinolone nucleus to increase antimicrobial activity and improve pharmacokinetic performance (12,22,29,46).The efficacy of fluoroquinolone antibiotics has led to their proposed use for the treatment and prophylaxis of different bacterial diseases: therapy for the respiratory tract, skin structure, and bone and gastrointestinal infections, as well as urinary tract infections (20,21,23,36,41). However, many studies were developed to improve the potency and spectrum, to achieve sustained blood levels, and to reduce as much as possible drug interactions with various metabolic pathways and physiological processes. Particularly, the use of antibiotic "carrier/delivery systems" would result in enhanced concentrations of the antimicrobial agent at the site of infection. In fact, delivery systems can contribute to (i) targeting of the drug to the infected tissues, (ii) increasing intracellular antibiotic concentrations, and (iii) reducing toxicity of potentially toxic drugs resulting from the targeting to the infectious organisms.Liposomes are possible carriers for controlled drug delivery and targeting by the intravenous route. As with most drug carriers, liposomes have been extensively used in an attempt to improve the selective delivery and the therapeutic index of antimicrobial agents (3, 47). Liposomes, artificial phospholipid membranes, are usually produced from naturally occurring, biodegradable, and nontoxic lipids, such as lecithin, cholesterol, and phosphatidylserine.The aim of the study described here was to investigate the antimicrobial activity against and accumulation in bacteria of ofloxacin-loaded liposomes (of different lipid compositions) in comparison to those of free drugs. Our preliminary experi...

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Section: Resultsmentioning

confidence: 99%

Ofloxacin-Loaded Liposomes: In Vitro Activity and Drug Accumulation in Bacteria

Furneri¹,

Fresta

Puglisi

et al. 2000

Antimicrob Agents Chemother

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“…Parameters for in vitro characterization of different liposomal formulations include size, shape, size distribution, entrapment efficiency and in vitro drug release profile. It is earlier reported that mean size of a colloidal drug carrier is an important requisite that may influence the in vivo performance of delivery system [40]. In order to obtain liposome colloidal suspensions with a reduced mean size, the sonication with probe sonicator was carried out.…”

Section: Discussionmentioning

confidence: 99%

A Novel Cancer Targeting Approach Based on Estrone Anchored Stealth Liposome for Site-Specific Breast Cancer Therapy

Paliwal¹,

Paliwal²,

Mishra³

et al. 2010

CCDT

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We here report the successful utilization of estrogen receptor (ER) for the delivery of anticancer drug doxorubicin (DOX) encapsulated within pegylated liposome for the treatment of breast cancer. Estrone (ES) was anchored as ligand on to stealth liposome (ES-SL-DOX) for targeting to ERs. In vitro cytotoxicity study was conducted on ER positive and negative breast carcinoma cells. The fluorescent microscopy studies were performed with estrone anchored stealth liposome (ES-SL) loaded with 6-carboxyfluorescein (6-CF). Pharmacokinetic, tissue distribution studies and tumor growth inhibition were carried out followed by intravenous (i.v.) administration of liposomal formulations. ES-SL-DOX demonstrated strongest cytotoxicity to the ER positive cell lines as compared to non-targeted formulations i.e. SL-DOX and plain DOX confirming that ES-SL-DOX was effectively taken up by cells expressing ERs. The half-life (t(1/2)) of SL-DOX and ES-SL-DOX was about 9 and 13 fold higher than that of the free DOX, respectively. Accumulation of ES-SL-DOX in the tumor tissue was 24.27 and 6.04 times higher as compared to free DOX and SL-DOX respectively, after 8 h. ES-SL-DOX at a dose of 5 mg DOX/kg resulted in effective retardation of tumor growth. These findings support that estrogen receptor(s) may be utilized as potential target for chemotherapy of cancers and estrone anchored stealth liposomes could be one of the promising solutions for the delivery of anticancer agent to breast tumors with reduced side-effects.

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“…Parameters for in vitro characterization of different liposomal formulations include size, shape, size distribution, zeta potential, entrapment efficiency, and in vitro drug release profile. As reported previously, mean size and zeta potential of a colloidal drug carrier are important parameters that influence the in vivo performance of delivery systems (Karajgi et al 1993). In order to obtain liposome colloidal suspensions with a reduced mean size, sonication was carried out with a probe sonicator.…”

Section: Discussionmentioning

confidence: 99%

Targeted delivery of doxorubicin via estrone-appended liposomes

Rai

Paliwal

Vaidya

et al. 2008

Journal of Drug Targeting

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Estrone-appended liposomal formulation of doxorubicin was designed to enhance the capability of clinically used liposomal doxorubicin formulation with the added advantage of delivery of doxorubicin to its destination site, i.e. cancerous cells overexpressing estrogen receptors (ERs). Estrone was conjugated with distearoyl phosphatidylethanolamine (DSPE) using succinic anhydride as a linker and the conjugate was characterized by IR and mass spectroscopies. Estrone-coupled liposomes were prepared with the composition of egg phosphatidylcholine/cholesterol/distearoyl phosphatidylethanolamine -estrone (PC/CHOL/DSPE -ES) at the molar and drug-lipid ratios of 7:3:0.5 and 0.1:1 (w/w), respectively. The average vesicle sizes of the conventional and estrone-appended liposomes were found to be 193^24 and 207^28 nm, respectively. The fluorescent microscopy studies were performed with estrone-appended liposomes loaded with 6-carboxyfluorescein (6-CF). Results of in vivo biodistribution studies showed that estrone-appended liposomes were effectively taken up by cells expressing ERs. The drug uptake study showed that accumulation of ligand-appended liposomes in the breast and uterus was 13.9 and 12.7 times higher when compared with plain drug, and 11.05 and 10.3 times higher when compared with conventional liposomes, respectively, after 8 h of tail vein intravenous administration. The findings are seminal for selective targeting of antineoplastic agents to the ER, which are frequently over-expressed on carcinoma of breast and uterine origin, and opens the promising possibilities for non-immunogenic, site-specific delivery of bioactive(s) to these sites.

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Passive Vectoring of a Colloidal Carrier System for Sodium Stibogluconate: Preparation, Characterization and Performance Evaluation

Cited by 11 publications

References 19 publications

Ofloxacin-Loaded Liposomes: In Vitro Activity and Drug Accumulation in Bacteria

Ofloxacin-Loaded Liposomes: In Vitro Activity and Drug Accumulation in Bacteria

A Novel Cancer Targeting Approach Based on Estrone Anchored Stealth Liposome for Site-Specific Breast Cancer Therapy

Targeted delivery of doxorubicin via estrone-appended liposomes

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