I've been searching for cationic materials to stabilize a suspension of drug nanocrystals. We want to prepare curcumin nanocrystals (with a bottom up approach, probably) but we need them to be cationic for application purposes (targeting to dendritic cells - immunotherapy). I've found chitosan, cationic surfactants, and other cationic polymers to be a good choice to stabilize nano and microcrystals for this highly hydrophobic drug. Do you have any information about this topic or do you personally know which one would be better in term of prevent changes in size and polydispersity of the system? Thanks a lot!
PD: do you also think cellulose nanocrystals with curcumin are also a good option?
dear
i dont have any idea about this but share your question with 2 man that are specialist in this.
i hope it will help you.
good luck
Hi,
Lets take it step by step.
Does it need to be necessarily cationic?
Your question can be clarified much better if we know the answer to this question.
Many ingredients can be suggested if you are not limited to use cationic agents.
For instance, 3 transdermal curcumin formulations and their ingredients are described below:
Curcumin propylene glycol liposome (PGL) preparation. Hydrogenated phosphatidylcholine 10 mg (HPC), cholesterol 5 mg (Chol), Tween-80 1 mg and curcumin 3 mg were added into propylene glycol. Then 7 ml 5% trehalose solution was added slowly into 3 ml propylene glycol solution with constant rotation of 750 r/min. Curcumin PGL was formed in solution after 10 min constant rotation.
Curcumin liposome preparation. Curcumin liposomes were prepared by ethanol injection method with the same component proportion as curcumin PGL. HPC, Chol, Tween 80 and curcumin were dissolved in 3 ml anhydrous ethanol. Then ethanol solution was added slowly into 10 ml distilled water with constant rotation. Ethanol in final liposome solution was removed by vacuum rotation evaporator. Curcumin liposome was formed after the removal of ethanol.
Curcumin ethosome preparation. Curcumin liposomes were prepared by ethanol injection method with the same component proportion as curcumin PGL. HPC, Chol, Tween 80 and curcumin were dissolved in 3 ml anhydrous ethanol. Then ethanol solution was added slowly into 7 ml distilled water with constant rotation with constant rotation of 750r/min. Curcumin ethosome was formed in solution after 10 min constant rotation.
Source:
Zhao YZ, Lu CT, Zhang Y, Xiao J, Zhao YP, Tian JL, Xu YY, Feng ZG, Xu CY. Selection of high efficient transdermal lipid vesicle for curcumin skin delivery. International journal of pharmaceutics. 2013 Sep 15;454(1):302-9.
With respect of SIZE considerations for transdermal (and sub-cutaneous) drug delivery I can refer you to this recent publication (published about a month ago):
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.
2.4. Impact of Particle Size on Transdermal Drug Delivery
Transdermal delivery of therapeutic agents involves the application of the formulation to the intact skin and delivery of the drug at a controlled rate locally or to the systemic circulation. As a convenient route of drug administration, transdermal drug delivery has made an important contribution to medical practice. However, it has yet to achieve its full potential as an alternative to oral delivery and hypodermic injections [51]. The mechanisms involved in transdermal drug delivery applications depend on the formulation of nanocarriers; in particular, factors such as chemical composition, surface charge, number of lamella and particle size must be carefully considered. The first studies on exploring the potential use of lipid vesicles in topical applications for the skin were reported in the 1980s [52,53,54]. Phospholipid vesicles have proven to be useful in the treatment of skin diseases such as psoriasis and skin cancer [55]. .......
Hi Dr. Mozafari for your answer.
1. We want them cationic because we are going to compare them with cationic liposomes. Also, we want a passive targeting to dendritic cells for immunomodulation purposes.
2. We want to stabilize crystals, not liposomes or other type of nanoparticles. I'm talking about a suspension of nano/microcrystals, stabilized by a cationic compound such polylysine, chitosan, CTAB, and others. But my question is that I'm not sure which would be the best cationic stabilizer for our crystals.
3. Tween 80 is a good option but it makes them anionic.
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