Drug targeting to lungs by way of microspheres

被引:25
作者
Harsha, N. Sree
Rani, R. H. Shobha
机构
[1] CNK Reddy Coll Pharm, Dept Pharmaceut, Bangalore 560096, Karnataka, India
[2] Al Ameen Coll Pharm, Dept Pharmaceut, Bangalore 560027, Karnataka, India
关键词
ofloxacin; gelatin; microspheres; in vitro; in vivo; compartment model; lung-targeting;
D O I
10.1007/BF02969272
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
In many conventional drug delivery systems in vogue, failure to deliver efficient drug delivery at the target site/organs; is evident as a result, less efficacious pharmacological response is elicited. Microspheres can be derived a remedial measure which can improve site-specific drug delivery to a considerable extent. As an application, Lung-targeting Ofloxacin-loaded gelatin microspheres (GLOME) were prepared by water in oil emulsion method. The Central Composite Design (CCD) was used to optimize the process of preparation, the appearance and size distribution were examined by scanning electron microscopy, the aspects such as in vitro release characteristics, stability, drug loading, loading efficiency, pharmacokinetics and tissue distribution in albino mice were studied. The experimental results showed that the microspheres in the range of 0.32-22 mu m. The drug loading and loading efficiency were 61.05 and 91.55% respectively. The in vitro release profile of the microspheres matched the korsmeyer's peppas release pattern, and release at 1 h was 42%, while for the original drug, ofloxacin under the same conditions 90.02% released in the first half an hour. After i.v. administration (15 min), the drug concentration of microspheres group in lung in albino mice was 1048 mu g/g, while that of controlled group was 6.77 mu g/g. GLOME found to release the drug to a maximum extent in the target tissue, lungs.
引用
收藏
页码:598 / 604
页数:7
相关论文
共 17 条
[1]
Brime B, 2000, J MICROENCAPSUL, V17, P777
[2]
Radiolabelled biodegradable microspheres for lung imaging [J].
Delgado, A ;
Soriano, I ;
Sánchez, E ;
Oliva, M ;
Evora, C .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2000, 50 (02) :227-236
[3]
Dhanaraj S. A., 2001, Indian Journal of Pharmaceutical Sciences, V63, P196
[4]
QUANTITATIVE-EVALUATION OF TARGETED DRUG DELIVERY SYSTEMS [J].
GUPTA, PK ;
HUNG, CT .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1989, 56 (03) :217-226
[5]
HIMANGSHU B, 2004, J VET SCI, V5, P97
[6]
Studies on the poly(lactic-co-glycolic) acid microspheres of cisplatin for lung-targeting [J].
Huo, DJ ;
Deng, SH ;
Li, LB ;
Ji, JB .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2005, 289 (1-2) :63-67
[7]
ILLUM L, 1982, INT J PHARM, V12, P135
[8]
JIA KL, 1997, J PHARM SCI, V86, P891
[9]
CLEARANCE OF CE-14-LABELED MICROSPHERES FROM BLOOD AND DISTRIBUTION IN SPECIFIC ORGANS FOLLOWING INTRAVENOUS AND INTRA-ARTERIAL ADMINISTRATION IN BEAGLE DOGS [J].
KANKE, M ;
SIMMONS, GH ;
WEISS, DL ;
BIVINS, BA ;
DELUCA, PP .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1980, 69 (07) :755-762
[10]
Lung-targeting microspheres of carboplatin [J].
Lu, B ;
Zhang, JQ ;
Yang, H .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2003, 265 (1-2) :1-11