Evaluation of antitubercular drug insertion into preformed dipalmitoylphosphatidylcholine monolayers

Chimote, Geetanjali; Banerjee, Rinti

doi:10.1016/j.colsurfb.2007.10.010

Cited by 13 publications

(10 citation statements)

References 27 publications

(26 reference statements)

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“…They are biodegradable and biocompatible being the major components of the plasma membrane. Phospholipid-based systems have been developed to increase solubility and enhance dissolution rate and bioavailability of water-insoluble drugs, especially phytopharmaceuticals (17)(18)(19)(20). Furthermore, they have been investigated to reduce NSAID-induced gastrointestinal toxicity and hepatotoxicity (21).…”

Section: Introductionmentioning

confidence: 99%

In Vitro-In Vivo Evaluation of Novel Co-spray Dried Rifampicin Phospholipid Lipospheres for Oral Delivery

Singh¹,

Koduri²,

Bhatt³

et al. 2016

AAPS PharmSciTech

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Abstract. The objective of this study comprises of developing novel co-spray dried rifampicin phospholipid lipospheres (SDRPL) to investigate its influence on rifampicin solubility and oral bioavailability. Solid-state techniques were employed to characterize the liposphere formulation. SDRPL solubility was determined in distilled water. BACTEC 460TB System was employed to evaluate SDRPL antimycobacterial activity. The oral bioavailability of the lipospheres was evaluated in Sprague Dawley rats. Lipospheres exhibited amorphous, smooth spherical morphology with a significant increase (p < 0.001) in solubility of SDRPL (2:1), 350.9 ± 23 versus 105.1 ± 12 μg/ml and SDRPL (1:1) 306.4 ± 20 versus 105.1 ± 12 μg/ml in comparison to rifampicin (RMP). SDRPL exhibited enhanced activity against Mycobacterium tuberculosis, H37Rv strain, with over twofolds less minimum inhibitory concentration (MIC) than the free drug. Lipospheres exhibited higher peak plasma concentration (109.92 ± 25 versus 54.31 ± 18 μg/ml), faster T max (two versus four hours), and enhanced area under the curve (AUC 0-∞ ) (406.92 ± 18 versus 147.72 ± 15 μg h/L) in comparison to pure RMP. Thus, SDRPL represents a promising carrier system exhibiting enhanced antimycobacterial activity and oral bioavailability of rifampicin.

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Section: Introductionmentioning

confidence: 99%

In Vitro-In Vivo Evaluation of Novel Co-spray Dried Rifampicin Phospholipid Lipospheres for Oral Delivery

Singh¹,

Koduri²,

Bhatt³

et al. 2016

AAPS PharmSciTech

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“…The strongest insertion into DPPC monolayers occurred for the most hydrophobic molecule (rifampicin), followed by the hydrophilic drugs (ethambutol and isoniazid), respectively [169].…”

Section: Accepted Manuscriptmentioning

confidence: 99%

Interactions of bioactive molecules & nanomaterials with Langmuir monolayers as cell membrane models

et al. 2015

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“…Использование дипальмитоилфосфатидилхолина как липида легочного сурфактанта считают перспективным подходом в разработке систем доставки ПТП в легкие, способствующим лучшему проникновению в альвеолы за счет сродства к собственным альвеолярным фосфолипидам [18]. В последующей работе тех же авторов на монослое из этого фосфолипида установлена возможность встраивания рифампицина в фосфолипидный монослой, что, по их мнению, происходит и в липосомах [19]. Получена стабильная порошковая форма рифампицина в липосомах из соевого ФХ с холестерином (1:1) в высоких концентрациях (10 мМ ФХ), с 50% инкапсулированием лекарственного средства [20].…”

Section: включение противотуберкулезных препаратов в наночастицы и наunclassified

Nanoparticles as Drug Delivery System for Antituberculous Drugs

et al. 2013

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The increase of tuberculosis incidence in last decade stimulated elaboration of both new antituberculous drugs and also searches of optimizing delivery systems for existing drugs. It is determined by their side effects and low bioavailability of effective first line drug rifampicin. Various nanosystems for transport of antituberculous drugs are considered on the basis of various polymers, liposomes, lipid nanoparticles, nanoemulsios, nanosuspensions, dendrimers, cyclodextrines. Influence of drug incorporation into nanoparticles, most often for rifampicin, on pharmacokinetics and efficiency in tuberculosis models is discussed. The most of works are devoted to polymer nanoparticles for oral administration where increased circulation time and efficiency were shown. The best results were observed after drug inclusion into solid lipid nanoparticles. The liposomes formulations were investigated mostly for inhalation and injection administrations. Positive results were also observed. Authors underline the viability of incorporation of antituberculous drugs into phospholipid nanoparticles that may increase intestinal absorption and bioavailability. It is confirmed by authors’ own data that showed increase of rifampicin efficiency after their incorporation into such nanoparticles.

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Evaluation of antitubercular drug insertion into preformed dipalmitoylphosphatidylcholine monolayers

Cited by 13 publications

References 27 publications

In Vitro-In Vivo Evaluation of Novel Co-spray Dried Rifampicin Phospholipid Lipospheres for Oral Delivery

In Vitro-In Vivo Evaluation of Novel Co-spray Dried Rifampicin Phospholipid Lipospheres for Oral Delivery

Interactions of bioactive molecules & nanomaterials with Langmuir monolayers as cell membrane models

Nanoparticles as Drug Delivery System for Antituberculous Drugs

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