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- Title
Synthesis and Assessment of Lipid Nanovesicles for Efficient Transdermal Delivery of Hydrophilic Molecules.
- Authors
Singh, Mahendra; Lee, Kyung Eun; Vinayagam, Ramachandran; Kang, Sang Gu
- Abstract
The transdermal delivery of hydrophilic molecules through the dermis is a challenging task because of the various skin barriers. Thus, lipid nanovesicles, including liposomes, ethosomes and transethosomes, are advantageous to transdermal drug delivery. This study was designed to develop nanovesicles like liposomes (LF1), ethosomes (EF1) and transethosomes (TF1) containing hydrophilic agents such as Rhodamine B (RB) as a model compound. Nanovesicles loaded with RB were synthesized using an ethanol injection method followed by probe sonication (hot method). The nonsonicated nanovesicles had vesicle sizes ranging from 1 6 0. 2 ± 1 6. 1 1 to 6 8 8. 2 ± 3 5. 8 5 nm, while sonicated nanovesicles sizes ranged from 8 2. 5 9 ± 9. 7 4 to 2 9 3. 6 ± 1 5. 8 5 nm. In addition, the nonsonicated nanovesicles had polydispersity index (PdI) ranging from 0. 2 3 8 ± 0. 0 2 2 to 1. 0 0 ± 0. 1 4 4 , whereas the PdI of the sonicated nanovesicles ranged from 0. 2 4 6 ± 0. 0 1 4 to 0. 4 6 2 ± 0. 0 9 4. Transmission electron microscopy revealed the distinguishable features of the sonicated nanovesicles depending on the compositions. The entrapment efficiency of RB was observed in the order of TF1 > EF1 > LF1. At the end of 10 h, RB permeated through the Strat-M ® membrane at 3. 1 8 8 ± 0. 8 9 0 , 4. 6 9 ± 0. 7 3 0 and 8. 6 4 4 ± 1. 0 8 0 μ g/cm2 from the LF1, EF1 and TF1 containing RB, respectively. The flux ( J SS ) of TF1 was obtained 5.53 times higher than RB itself. Therefore, the TF1 nanovesicle allowed the highly efficient permeation and entrapment of hydrophilic RB compared to LF1 and EF1 nanovesicles. Hence, it can be concluded that transethosomes would be a better choice for hydrophilic compounds to cross the skin barriers via the transdermal route. The research aimed to prepare and characterize the three lipid nanovesicles, i.e., liposomes, ethosomes and transethosomes, for efficient transdermal delivery of hydrophilic model molecules. The prepared formulations were evaluated for structural morphology by using SEM, globule sizes (Zeta sizer), entrapment efficiency and comparative permeability studies. Transethosomes were showed better permeability than liposomes and ethosomes.
- Subjects
LIPID synthesis; MOLECULES; TRANSDERMAL medication; TRANSMISSION electron microscopy; RHODAMINE B; ETHANOL
- Publication
NANO, 2022, Vol 17, Issue 4, p1
- ISSN
1793-2920
- Publication type
Article
- DOI
10.1142/S179329202250031X