I am developing a procedure for liposome formulation,
the best two results I have, regarding the size, are: 21 (+/- 8) nm and 68 (+/- 36) nm. Which one is the best for drug encapsulation for health and food applications?
It depends on many factors, including route of administration, size of drug (or any other bioactive) to be encapsulated, selection of liposomal / nanoliposomal ingredients (which are mainly phospholipids with / without sterols and antioxidants), ... as explained in the attached paper.
Please note: Submicron "Liposomes" are called "Nanoliposomes" (refer to the relevant literature listed below).
[Nanoliposomes: From Fundamentals to Recent Developments
Book by M. R. Mozafari]
Mozafari, M.R. & Mortazavi, S.M. (2005) Nanoliposomes: From Fundamentals to Recent Developments. Trafford Publishing Ltd, Oxford, UK. ISBN 1-4120-5545-8
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Danaei, M.; Dehghankhold, M.; Ataei, S.; Hasanzadeh Davarani, F.; Javanmard, R.; Dokhani, A.; Khorasani, S.; Mozafari, M.R. Impact of Particle Size and Polydispersity Index on the Clinical Applications of Lipidic Nanocarrier Systems. Pharmaceutics 2018, 10, 57.
As I said previously, according to researcher purpose and expectation, the size ranges of liposomes are variable. For example, the size more than 200 nm is not proper for drug delivery (due to diameter size of cancer tissue's micro-vascular); however, the size range of NPs for food applications can be more than 300 to 400 nm (due to loading capacity of nanocarrier). Therefore, as I said previously, it directly related to practical applications of synthetic liposomes in a way that researcher follows.
Thank you very much for your valuable advice and shared papers!
Dear Dr. Patel and Dr. Mozafari,
The drugs being encapsulated are small and hydrophile. Considering your opinions, I would chose the 68 nm liposomes rather than 21 nm one. The other factor which made me hesitate is the polydispersity index (PDI, 0.27 and 0.14 respectively). Obviously, less the liposomes are polydisperse more the pharmacokenitic parameters are significant. However, PDI of 0.27 still good (matching most of the literature data I've read), 68 nm small enough, so the curvature stress effect seems to be considered more. Isn't it?!
By the way, I am willing to add cholesterol into the formulation for the first time (to decrease the leakage of the drug in time), How do you expect its effect on the size?