1. Well-deﬁned PCL-graft-PDMAEMA prepared by ring-opening polymerisation and click chemistry
Vincent Darcos,* Sarah El Habnouni, Benjamin Nottelet, Abdeslam El Ghzaoui and Jean Coudane. Polym. Chem., 2010, 1, 280–282
When used as drug carriers in aqueous media, polymeric micelles are capable of encapsulating hydrophobic drugs in their core, thus improving the drug water solubility. The quaternized graft copolymer micelles were used to solubilise an anti-mycobacterial drug, the clofazimine (Fig. 3). This drug has the disadvantage of being highly hydrophobic with inherent water solubility below 0.3 mgmL-1 and Log P = 7.5. The aqueous graft copolymer solution where the concentration is above the CMC present a different behaviour in comparison with water and copolymer solution below the CMC. A deep red colour appears in copolymer solution where the concentration is above the CMC, which means that clofazimine was well solubilised. But, as the copolymer concentration decreases and becomes slightly lower than the CMC, the red colour becomes less lively as a consequence of the strong decrease in the clofazimine solubilisation.
2. An insight into cochleates, a potential drug delivery system
Atmaram Pawar, C. Bothiraja,* Karimunnisa Shaikh and Ashwin Mali. RSC Adv.,2015, 5, 81188–81202
The antibacterial agent like clofazimine, aminoglycosides, beta-lactam/beta-lactamase combinations, vancomycin, imipenem and ethionamide require long term treatment, thereby produce toxicity and drug resistance in host. Cochleates can reduce toxicity and improve their bactericidal activity. It was proved by a study on clofazimine cochleates which were prepared by trapping method and whose safety and eﬃcacy was analysed in cell culture. It was concluded that clofazimine cochleate was 500 times less toxic than free clofazimine.
3. The Medicinal Chemistry of Anti-leprosy Drugs
M. Hooper. Chem. Soc. Reu., 1987, 16, 437465
These are dapsone, rifampicin, and clofazimine. Until recently, extensive and often life-long monotherapy, particularly with dapsone, the first effective anti-leprosy drug, was commonplace. The emergence of resistant organisms as secondary (occurring during therapy) or primary (the original infection) resistance coupled with the recognition that shorter term therapy gains wider patient compliance has led to the current use of multi-drug treatment regimens. The proposed drug regimens vary somewhat with the clinical classification of the disease. Standard regimens proposed by the WHO THELEP pane119 are now being evaluated worldwide, but other regimens are also being used. Generally, for lepromatous leprosy, rifampicin (the most potent bactericidal drug) is used with dapsone and clofazimine or prothionamide over a five year period. For tuberculoid leprosy, two drugs, rifampicin and either dapsone or clofazimine, over two to three years are recommended. The interactions of these drugs in vivo is an imporant area of investigation.