Optimisation of chloroquine phosphate loaded nanostructured lipid carriers using Box–Behnken design and its antimalarial efficacy

Abstract

Chloroquine was once the most widely used antimalarial for nearly eight decades for its safety, efficiency, stability, low cost and finally for its less toxic nature. But its use and efficacy got slowly decreased with the increase of chloroquine resistant strains of Plasmodium species throughout the world. Lipid based nanodrug delivery systems have been very popular in the recent times as they are very less toxic, have drug targeting capabilities and also reduces the dosing frequency by increasing efficacy of the drug. In the present research work, response surface methodology was employed to optimise chloroquine phosphate (CQ) loaded nanostructured lipid carriers (NLCs) using a modified double emulsion technique. The optimised CQ loaded NLC showed a particle size of 66.50 ± 1.21 nm, PDI of 0.210 ± 0.016, ZP of +38.4 ± 1.44 and EE of 78.2 ± 1.2%, respectively. The in vitro and in vivo antimalarial studies of CQ loaded NLCs showed an enhanced antimalarial efficacy of the nanoformulation with a better suppression of parasitemia and with an increased efficacy of more than 23% in comparison to pure drug. This study demonstrated that by loading a drug into an NLCs system can help in overcoming the problems associated with the present antimalarials available.

Pharmaceutical care of chloroquine phosphate in elderly patients with coronavirus pneumonia (COVID‐19)

“…In 1944, scientists modified the structure of chloroquine by adding a hydroxyl group to it, and developed a new antimalarial drug, hydroxychloroquine, which was less toxic and more effective against malaria. 5 At present, two independent experiment teams from China have confirmed that chloroquine has an impact against the SARS virus in vitro. 6 At present, the safety of chloroquine phosphate in the treatment of elderly patients with COVID-19 cannot be determined, but the rate of critical illness in the elderly is high and chloroquine phosphate can still be used as an alternative antiviral drug for the elderly.…”

Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization

“…The mixture was centrifuged at 15,000 rpm for 30 min at 25 ± 0.5 • C by a centrifuge (model 2-16P, Sigma, Osterode am Harz, Germany) to separate the lipid. The resultant supernatant (aqueous phase) was diluted in order to quantify the amount of AT using a UV spectrophotometer (Tokyo, Japan) [21] The partition coefficient (Log P) was then calculated using the following equation [22]: PC = log Added drug content − Drug content in aqueous phase Drug content in aqueous phase (1)…”

“…Samples were transferred from the shaker to a centrifugation machine and centrifuged at 15,000 rpm for 30 min. To filter the supernatant, a 0.22 µm membrane filter (HiMedia, Mumbai, India) was used [21]. The filtered supernatant was assayed by a UV spectrophotometer.…”

Novos sistemas de delivery, uso tecnológico e reposicionamento da cloroquina e hidroxicloroquina: Uma revisão integrativa

“…Dessa forma, é imprescindível e impreterível a criação de novas estratégias de tratamento para a malária. Nesse contexto, como o processo de pesquisa e desenvolvimento de drogas demanda um tempo considerável, a reformulação dos antimaláricos disponíveis, por meio do uso de novos sistemas de delivery, pode ser considerada uma solução viável e menos dispendiosa de tempo e recursos (Baruah et al, 2018;Medhi et al, 2018;Rajendran et al, 2017).…”