“…the skin (3). Transfersomes incorporate edge activators (surfactants) which destabilize lipid bilayers and increase deformability of the vesicles (4).…”
Transdermal delivery of drugs offers many advantages compared to traditional drug delivery systems, including oral and injectable preparations. Due to their amphiphilic nature, lipid vesicles may serve as non-toxic penetration enhancers for drugs (1, 2). However, this approach is not very successful because of poor skin permeability, breaking of vesicles, drug leakage, aggregation and fusion of vesicles. To overcome problems of poor skin permeability, a novel vesicular system, transfersomes (ultradeformable lipid vesicles) were proposed for non-invasive delivery of drugs into deep skin strata or across Cisplatin-loaded protransfersome system was prepared and characterized for in vitro drug permeation, drug deposition and antitumor effect. A histopathological study and a genotoxicity study were also done. The skin permeation data of cisplatin from protransfersome gel formulation revealed 494.33 ± 11.87 mg cm -2 , which was significantly higher than that from the control plain drug solution in 0.9 % NaCl (p < 0.001). Untreated group of animals showed invasive moderately differentiated keratinizing squamous cell carcinoma (malignant stage). However, with cisplatin loaded protransfersome gel system simple epithelial hyperplasia (pre-cancerous stage) with no cancerous growth was observed. Also, a significant induction in micronucleus formation was found in the group that was treated with injectable intraperitoneal cisplatin preparation in 0.9 % saline as compared to the group treated with topical protransfersome gel formulation. The findings of this research work appear to support improved, site-specific and localized drug action in the skin, thus providing a better option for dealing with skin related problems like squamous cell carcinoma.
“…the skin (3). Transfersomes incorporate edge activators (surfactants) which destabilize lipid bilayers and increase deformability of the vesicles (4).…”
Transdermal delivery of drugs offers many advantages compared to traditional drug delivery systems, including oral and injectable preparations. Due to their amphiphilic nature, lipid vesicles may serve as non-toxic penetration enhancers for drugs (1, 2). However, this approach is not very successful because of poor skin permeability, breaking of vesicles, drug leakage, aggregation and fusion of vesicles. To overcome problems of poor skin permeability, a novel vesicular system, transfersomes (ultradeformable lipid vesicles) were proposed for non-invasive delivery of drugs into deep skin strata or across Cisplatin-loaded protransfersome system was prepared and characterized for in vitro drug permeation, drug deposition and antitumor effect. A histopathological study and a genotoxicity study were also done. The skin permeation data of cisplatin from protransfersome gel formulation revealed 494.33 ± 11.87 mg cm -2 , which was significantly higher than that from the control plain drug solution in 0.9 % NaCl (p < 0.001). Untreated group of animals showed invasive moderately differentiated keratinizing squamous cell carcinoma (malignant stage). However, with cisplatin loaded protransfersome gel system simple epithelial hyperplasia (pre-cancerous stage) with no cancerous growth was observed. Also, a significant induction in micronucleus formation was found in the group that was treated with injectable intraperitoneal cisplatin preparation in 0.9 % saline as compared to the group treated with topical protransfersome gel formulation. The findings of this research work appear to support improved, site-specific and localized drug action in the skin, thus providing a better option for dealing with skin related problems like squamous cell carcinoma.
“…These findings suggested that the combined effect of improved skin permeation was the reason for the success of such molecules. 78 Recently, 5-FU was formulated in thermosensitive stealth liposomes (TSLs) and the pharmacokinetic profile was determined by triggering drug release upon hyperthermia by using ultrasound as a physical method. Complexing 5-FU with copper polyethylenimine appeared to be an attractive strategy to improve 5-FU retention in TSLs in vitro and in vivo.…”
Elastic liposomes (EL) are some of the most versatile deformable vesicular carriers that comprise physiologically biocompatible lipids and surfactants for the delivery of numerous challenging molecules and have marked advantages over other colloidal systems. They have been investigated for a wide range of applications in pharmaceutical technology through topical, transdermal, nasal, and oral routes for efficient and effective drug delivery. Increased drug encapsulation efficiency, enhanced drug permeation and penetration into or across the skin, and ultradeformability have led to widespread interest in ELs to modulate drug release, permeation, and drug action more efficiently than conventional drug-release vehicles. This review provides insights into the versatile role that ELs play in the delivery of numerous drugs and biomolecules by improving drug release, permeation, and penetration across the skin as well as stability. Furthermore, it provides future directions that should ensure the widespread use of ELs across all medical fields.
“…It has significant activity in the treatment of breast, nonsmall-cell lung, ovarian, and head and neck cancers (Clarke & Rivory, 1999). Because of the bulky, extended fused ring with several hydrophobic substitutes in chemical structure, DTX provides high lipophilicity (log P ¼ 4.1) (Mastropaolo et al, 1995;Carstens et al, 2008) with very poor aqueous solubility (6-7 mg/mL) (Du et al, 2007;Qiu et al, 2008), which limits its clinical use.…”
Docetaxel is one of the most active chemotherapeutic agents for cancer treatment. The traditional docetaxel injection (TAXOTERE Õ ) is currently formulated in the surfactant polysorbate 80, which has been associated with severe adverse reactions. To avoid the use of polysorbate 80 as well as to reduce the systemic toxicity of docetaxel, in this study, docetaxel-loaded albumin nanoparticles were fabricated by a novel simple self-assembly method. The resulting nanoparticles showed a mean diameter size of 150 nm. After being encapsulated into nanoparticles, docetaxel displayed similar cytotoxicity to traditional injection. Since polysorbate 80 was not involved in nanoparticles, the hemolysis was completely eliminated. The maximal tolerance dose of nanoparticles was also increased, which allowed a higher dose to be safely intravenously injected and produced ideal antitumor effects. The 150 nm diameter also allowed the nanoparticles to accumulate in tumor tissue via the enhanced permeability and retention effect. The passive targeting ability further caused the higher antitumor effects of nanoparticles than that of traditional injection at the same dose (7.5 mg/kg). Therefore, docetaxel-loaded albumin nanoparticles fabricated by our strategy showed higher promise in their safety and effectiveness than the traditional docetaxel injection.
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