Formulation and optimisation of bedaquiline nanoemulsions for the potential treatment of multi drug resistant tuberculosis in paediatrics using quality by design.

Publication date: Dec 30, 2024

Bedaquiline is a drug used for the treatment of multidrug-resistant TB in adults and children that is currently only commercially available in tablet form. The present study was aimed at preparing nanoemulsion (NE) of BDQ using natural vegetable oils to deliver BDQ. The optimisation of surfactant mixtures was undertaken using Design of Experiments (DoE), specifically an optimal mixture design. The NEs were optimised while monitoring droplet size (DS), zeta potential (ZP), polydispersity index (PDI) and drug content (DC). The optimised NEs were further characterised using transmission electron microscopy, electrical conductivity, viscosity, pH and in vitro release studies. The optimised NE showed values of 191. 6 nm +/- 2. 38 nm, 0. 1176 +/- 1. 69, -25. 9 mV +/- 3. 00 mV and 3. 14 +/- 0. 82 mg/ml for DS, PDI, ZP and DC respectively. Furthermore, the TEM studies demonstrated the spherical shape of the optimised globules. The nanoemulsion was characterised by measuring its electrical conductivity, viscosity and pH which were determined as 53. 1 uS/cm, 327 +/- 3. 05 cP and 5. 63 +/- 1. 78, respectively. In conclusion, these NEs have great potential for improving solubility, drug delivery, and administration of BDQ. However, further studies are required to maximise the drug content and to demonstrate to what extent these NE have effect against MDR-TB.

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Concepts Keywords
Bedaquiline Antitubercular Agents
Drugs Antitubercular Agents
Nanoemulsion bedaquiline
Paediatrics Bedaquiline
Vegetable Child
Diarylquinolines
Diarylquinolines
Droplet size
Drug Compounding
Drug Release
Emulsions
Emulsions
Humans
Hydrogen-Ion Concentration
Multi-Drug-Resistant Tuberculosis
Nanoemulsions
Nanoparticles
Particle Size
Quality by Design
Tuberculosis, Multidrug-Resistant
Viscosity
Zeta potential

Semantics

Type Source Name
drug DRUGBANK Bedaquiline
disease MESH tuberculosis
pathway KEGG Tuberculosis
disease IDO quality
pathway REACTOME Release
drug DRUGBANK Tretamine
drug DRUGBANK Isoniazid
drug DRUGBANK Rifampicin
drug DRUGBANK Delamanid
drug DRUGBANK Moxifloxacin
drug DRUGBANK Levofloxacin
drug DRUGBANK Clofazimine
drug DRUGBANK Ethambutol
drug DRUGBANK Ethionamide
drug DRUGBANK Pyrazinamide
drug DRUGBANK ATP
disease IDO production
pathway REACTOME Metabolism
disease IDO blood
drug DRUGBANK Coenzyme M
drug DRUGBANK Water
drug DRUGBANK Venetoclax
drug DRUGBANK Vemurafenib
drug DRUGBANK Benidipine
drug DRUGBANK Ethanol
drug DRUGBANK Olive oil
drug DRUGBANK Isoxaflutole
disease IDO process
drug DRUGBANK Acetic acid
drug DRUGBANK Copper
drug DRUGBANK Methionine
drug DRUGBANK Abacavir
drug DRUGBANK Esomeprazole
drug DRUGBANK Polysorbate 80
drug DRUGBANK Spectinomycin
drug DRUGBANK Alpha-1-proteinase inhibitor
drug DRUGBANK Flunarizine
disease MESH extensively drug resistant tuberculosis
drug DRUGBANK Phenobarbital
drug DRUGBANK Danazol
disease IDO cell
drug DRUGBANK Phytosphingosine
drug DRUGBANK Amlodipine
drug DRUGBANK Dexibuprofen
drug DRUGBANK Amikacin
drug DRUGBANK Diethylstilbestrol
drug DRUGBANK Vitamin E
pathway REACTOME Vitamin E transport
drug DRUGBANK Naltrexone
drug DRUGBANK L-Aspartic Acid
disease IDO protein
disease MESH Hards
drug DRUGBANK Alginic acid
drug DRUGBANK Lidocaine
drug DRUGBANK Centella asiatica
drug DRUGBANK Naloxone
drug DRUGBANK Propranolol
drug DRUGBANK Artemether
drug DRUGBANK Curcumin
drug DRUGBANK Ramipril
drug DRUGBANK Diltiazem
pathway REACTOME Reproduction
disease MESH Drug-Resistant Tuberculosis

Original Article

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