Physicochemical Properties and Antifungal Activity of Amphotericin B Incorporated in Cholesteryl Carbonate Esters

Chuealee, Rabkwan; Wiedmann, Timothy S.; Srichana, Teerapol

doi:10.1002/jps.22398

Cited by 8 publications

(4 citation statements)

References 28 publications

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“…All the DPI formulations of AmB-CCE demonstrated greater in vitro antifungal activity against Crytococcus neoformans (ATCC 90113) and Candida albicans (ATCC 90028) as evidenced through the 2 to 4 times lower minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) compared to pure AmB. This was due to the synergistic effect provided by the liquid crystals with AmB in the inhibition of fungal growth as well as the facilitation of transfer or induction of ionophore formation as AmB drug molecules may be transported into the fungal cells together with the liquid crystal molecules [34]. The improvement of antifungal activity and aerosol performance of the DPI formulations using CCEs demonstrated their suitability to be used as carriers.…”

Section: Dry Powder Inhaler Formulationsmentioning

confidence: 99%

A Critical Review on Emerging Trends in Dry Powder Inhaler Formulation for the Treatment of Pulmonary Aspergillosis

et al. 2020

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Pulmonary aspergillosis (PA), a pulmonary fungal infection caused by Aspergillus spp., is a concern for immunocompromised populations. Despite substantial research efforts, conventional treatments of PA using antifungal agents are associated with limitations such as excessive systemic exposure, serious side effects and limited availability of the therapeutics in the lungs for an adequate duration. To overcome the limitations associated with the conventional regimens, pulmonary delivery of antifungal agents has become a focal point of research because of the superiority of local and targeted drug delivery. Dry powder inhalers and nebulized formulations of antifungal agents have been developed and evaluated for their capability to effectively deliver antifungal agents to the lungs. Moreover, progress in nanotechnology and the utilization of nanocarriers in the development of pulmonary delivery formulations has allowed further augmentation of treatment capability and efficiency. Thus, the following review provides an insight into the advantages and therapeutic potential of the utilization of nanocarriers in pulmonary delivery of antifungal agents for the treatment of PA. In addition, discussions on formulation aspects and safety concerns together with the clinical and regulatory aspects of the formulations are presented, which suggest the possibility and desirability of utilization of nanocarriers in the treatment of PA.

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Section: Dry Powder Inhaler Formulationsmentioning

confidence: 99%

A Critical Review on Emerging Trends in Dry Powder Inhaler Formulation for the Treatment of Pulmonary Aspergillosis

et al. 2020

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“…The dry powders produced were observed to be stable after 3 months of storage, and the MMAD was measured to be 6.8–8 μm. The powder was effective against C. neoformans and C. albicans , and further investigation of this form of encapsulation is warranted 65. In a study by Nasr et al,66 a lipid nanoemulsion containing amphotericin B aerosol was evaluated.…”

Section: Amphotericin Bmentioning

confidence: 99%

Clinical experimentation with aerosol antibiotics: current and future methods of administration

Zarogoulidis¹,

Kioumis²,

Porpodis³

et al. 2013

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Currently almost all antibiotics are administered by the intravenous route. Since several systems and situations require more efficient methods of administration, investigation and experimentation in drug design has produced local treatment modalities. Administration of antibiotics in aerosol form is one of the treatment methods of increasing interest. As the field of drug nanotechnology grows, new molecules have been produced and combined with aerosol production systems. In the current review, we discuss the efficiency of aerosol antibiotic studies along with aerosol production systems. The different parts of the aerosol antibiotic methodology are presented. Additionally, information regarding the drug molecules used is presented and future applications of this method are discussed.

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“…In view of the increased threat from these drugresistant Gram-positive and Gram-negative bacterial strains and also Candida strains, there is a continuous demand and perusal to identify new antimicrobial agents. Several reports claim that numerous potent biological activities such as, insect repellent 3 , antibacterial [4][5][6][7] , pesticidal 8 , antifungal [9][10][11] , anti-inflammation 12 , antioxidant…”

Section: Introductionmentioning

confidence: 99%

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2016

IJPSR

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A series of novel cholesteryl lactate-fatty acid conjugates (4a-i) were prepared by esterification of cholesterol with lactic acid, followed by coupling hydroxyl group of cholesteryl lactate with -COOH group of fatty acids including, saturated fatty acids of varying carbon chain of C 10 -C 18 , unsaturated fatty acids like 10-undecenoic, oleic ((9Z)-octadec-9-enoic), ricinoleic ((9Z,12R)-12-hydroxyoctadec-9-enoic) and 11-bromoundecanoic acid. Cholesteryl lactate-fatty acid conjugates were characterized by spectroscopic techniques like FT-IR, 1H-NMR, 13C-NMR, ESI-MS and HRMS. All the synthesized compounds were tested for their antimicrobial activity against a panel of seven bacterial strains like Staphylococcus aureus MTCC 96, Bacillus subtilis MTCC 121, Micrococcus luteus MTCC 2470, Klebsiella planticola MTCC 530, Escherichia coli MTCC 739, Pseudomonas aeruginosa MTCC 2453 and fungal strain like Candida albicans. Among them, the compounds with unsaturation (4f and 4h), and functional groups like bromine and hydroxyl group (4g and 4i) showed good antibacterial activity. But, promising activity was observed against Staphylococcus aureus MTCC 96 strain ranging from 7.8-15.6 µg/ml. These compounds (4f-i) are also exhibited good to moderate antifungal activity against different Candida strains ranging between 7.8-31.2 µg/ml.

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Physicochemical Properties and Antifungal Activity of Amphotericin B Incorporated in Cholesteryl Carbonate Esters

Cited by 8 publications

References 28 publications

A Critical Review on Emerging Trends in Dry Powder Inhaler Formulation for the Treatment of Pulmonary Aspergillosis

A Critical Review on Emerging Trends in Dry Powder Inhaler Formulation for the Treatment of Pulmonary Aspergillosis

Clinical experimentation with aerosol antibiotics: current and future methods of administration

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