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Published on: March 8, 2018
Targeted delivery of an anti-cancer agent via steroid coupled liposomes
Pramod K Mishra1, Arvind Gulbake, Aviral Jain
1Department of Pharmaceutical Sciences, UTD, SAGAR, India.
Abstract:
In the present investigation, testosterone (T) was evaluated as a targeting ligand to direct the site-specific delivery of 5-Fluorouracil (5-FU) bearing liposomes to the androgen receptor (ARs) positive tumors and other organs like prostate, brain, and testis. The testosterone was conjugated with the distearoyl phosphatidyl ethanolamine (DSPE) and then this lipid conjugate, Testosterone-DSPE (T-DSPE) was used as one of the components of the liposome. The liposomes were prepared by cast film method using T-DSPE, egg PC, and cholesterol. Further these liposomes were characterized for vesicle shape, average size, polydispersity index, drug entrapment, and in vitro drug release. It was observed that the prepared liposomes were spherical in shape with an average size of 232 +/- 21 nm and 0.181 +/- 0.064 polydispersity index. The in vitro drug release study showed 79.50 +/- 2.81 percent drug release in 24 h. In vivo performance of the developed liposomes was evaluated using organ distribution study in male albino rats. Moreover the fluorescent microscopy was also performed using 6-Carboxyfluorescein (6-CF) as a fluorescent marker. The organ distribution and fluorescent uptake studies confirm that T-DSPE coupled liposomes were effectively taken up by various ARs expressing tissues. Thus, it may be concluded that the testosterone may be used as an effective ligand for the site-specific delivery of anti-cancer agents to various ARs positive carcinomas.
Insights
Testosterone conjugated liposomes show targeted delivery of 5-Fluorouracil to androgen receptor-positive tumors. This approach enhances drug delivery to ARs-expressing tissues, offering potential for site-specific cancer therapy.
Area of Science:
- Nanomedicine
- Pharmacology
- Oncology
Background:
- Targeted drug delivery systems are crucial for enhancing the efficacy of chemotherapeutic agents like 5-Fluorouracil (5-FU).
- Androgen receptors (ARs) are overexpressed in various carcinomas, presenting a potential target for site-specific drug delivery.
Purpose of the Study:
- To evaluate testosterone (T) as a targeting ligand for liposomal delivery of 5-FU to AR-positive tumors.
- To develop and characterize testosterone-conjugated liposomes (T-DSPE) for enhanced delivery to AR-expressing tissues.
Main Methods:
- Liposomes were prepared using Testosterone-DSPE (T-DSPE), egg PC, and cholesterol via the cast film method.
- Liposomes were characterized for size, polydispersity index, drug entrapment, and in vitro drug release.
- In vivo organ distribution and fluorescent microscopy studies were conducted in male albino rats using 6-Carboxyfluorescein (6-CF).
Main Results:
- Prepared liposomes were spherical with an average size of 232 ± 21 nm and a polydispersity index of 0.181 ± 0.064.
- In vitro studies showed 79.50 ± 2.81% drug release within 24 hours.
- Organ distribution and fluorescent uptake studies confirmed effective uptake of T-DSPE liposomes by ARs-expressing tissues.
Conclusions:
- Testosterone-DSPE liposomes demonstrate efficient targeting and uptake in ARs-expressing tissues.
- Testosterone can serve as an effective ligand for site-specific delivery of anti-cancer agents to ARs-positive carcinomas.
- This targeted delivery approach holds promise for improving cancer treatment outcomes.
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