Transdermal delivery of isoniazid and rifampin in guinea pigs by electro-phonophoresis

Chen, Suting; Han, Yi; Yu, Dian; Huo, Fengmin; Wang, Fen; Li, Yunxu; Dong, Lingling; Liu, Zhidong; Huang, Hairong

doi:10.1080/10717544.2016.1267275

Cited by 9 publications

(8 citation statements)

References 11 publications

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“…Previous studies evaluated the transdermal delivery of INH/RIF and reported avoidance of the hepatic first-pass effect, which resulted in dose reduction and mitigation of side effects (peripheral neuropathy and hepatotoxicity). 10,12 Chen et al investigated transdermal delivery of RIF and INH using electro-phonophoresis for treatment of superficial skin tuberculosis and tubercular lymphadenitis. 12 However, these drugs were evaluated as components of a nanocarrier-based transdermal delivery system.…”

Section: Introductionmentioning

confidence: 99%

“…10,12 Chen et al investigated transdermal delivery of RIF and INH using electro-phonophoresis for treatment of superficial skin tuberculosis and tubercular lymphadenitis. 12 However, these drugs were evaluated as components of a nanocarrier-based transdermal delivery system.…”

Section: Introductionmentioning

confidence: 99%

“…Rifampicin (Log P~3.8) is the first-line treatment for pulmonary and tubercular lymphadenitis (cutaneous tuberculosis). 12 However, RIF has limited aqueous solubility (~1 mg/mL) and is a Class II drug according to the Biopharmaceutical Classification System. Therefore, RIF may be a promising candidate for augmented transdermal delivery using isotropic and thermodynamically stable nanoemulsions comprised of excipients that have innate anti-Mycobacterium activity.…”

Section: Introductionmentioning

confidence: 99%

“…Moreover, the SC augments the transdermal delivery of lipophilic drugs. 12,14 In our previous studies, excipients with innate activity against virulent and non-virulent strains of Mycobacterium were loaded with RIF in self-emulsifying formulations. These formulations exhibited improved dissolution rates and in vivo pharmacokinetic parameters following oral delivery.…”

Section: Introductionmentioning

confidence: 99%

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<p>Novel Approach for Transdermal Delivery of Rifampicin to Induce Synergistic Antimycobacterial Effects Against Cutaneous and Systemic Tuberculosis Using a Cationic Nanoemulsion Gel</p>

Hussain¹,

Altamimi²,

Alshehri³

et al. 2020

IJN

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This study demonstrated improved transdermal delivery of rifampicin-loaded cationic nanoemulsion gel to treat systemic and cutaneous tuberculosis using capmul, labrasol, and acconon, which exert anti-Mycobacterium activities. This approach enhanced drug permeation across the skin, increased therapeutic efficacy, and reduced dose-related side effects. Methods: Design Expert ® was used to optimize formulations (S mix ratio and capmul as independent factors), which were prepared using a slow spontaneous titration method. The optimized nanoemulsion was incorporated into carbopol gel to allow for topical application and comparative assessments. Nanoemulsions and gels were evaluated for size, size distribution, shape, zeta potential, percent spread, viscosity, in vitro hemolysis, in vitro release, and ex vivo skin permeation and deposition. A mechanistic evaluation was performed using scanning electron microscopy. Furthermore, in vivo pharmacokinetic and irritation studies were performed. Results: The optimized cationic nanoemulsion (OCNE-1) was characterized by small particle size (≤100 nm), had optimal viscosity, percent spread, zeta potential, and percent drug release, and was hemocompatible. The OCNE-1T gel exhibited higher permeation flux (51.32 ± 0.5 µg/cm 2 hr), permeation coefficient (2.566 ± 0.08 cm/hr), drug deposition (994.404 µg/cm 2), and enhancement ratio (7.16) than those of the OCNE-1 nanoemulsion or drug solution. Scanning electron microscopy was used to characterize the mechanism of enhanced permeation. An In vivo study showed that the C max and area under the curve following transdermal application were 4.34-and 4.74-fold higher than those following oral administration. Conclusion: Transdermal delivery of rifampicin could be a promising alternative to conventional approaches to treat systemic and local tuberculosis, and other bacterial infections.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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<p>Novel Approach for Transdermal Delivery of Rifampicin to Induce Synergistic Antimycobacterial Effects Against Cutaneous and Systemic Tuberculosis Using a Cationic Nanoemulsion Gel</p>

Hussain¹,

Altamimi²,

Alshehri³

et al. 2020

IJN

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“…INH gets converted to isonicotinic acid due to radicalmediated chain reaction (Bhutani et al).It comes under borderline of BCS Class I and Class III drugs with good aqueous solubility of (140000 mg/L at 25°C), Log P -0.71(hansch, ceta1995) and pKa of 1.82 at 20°C (Perrin, DD 1965). It is a bactericidal drug and acts by inhibiting biosynthesis of mycolic acid which is major component of bacterial cell wall 6 . The drug faces various stability problems like hydrolysis, oxidation and photolysis, forming isonicotinic acid and isonicotinamide.…”

Section: Mycobacteriummentioning

confidence: 99%

Formulation and Evaluation of Topical Formulation for Cutaneous Tuberculosis

Rao¹,

Kadam²,

Rao³

2018

J. Drug Delivery Ther.

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Cutaneous Tuberculosis is also known as dermal tuberculosis or tuberculosis cutis (extrapulmonary tuberculosis) which can occur in any age group and patients who may or may not be suffering from pulmonary tuberculosis. The current treatment given for the disease is oral therapy of anti-tubercular drugs which has many side effects such as hepatotoxicity, headache, anxiety, euphoria, insomnia, eosinophilia, hepatitis. Hence to avoid these side effects and to increase efficiency of current therapy a topical proniosomal gel of isoniazid was formulated. Coacervation phase separation method was used and proniosomal gel was formulated by using Span 20, soya lecithin, and cholesterol. Optimum concentration of 3 factors Span 20, soya lecithin, and cholesterol were determined using Box Behnken design with at 2 levels and vesicle size and entrapment efficiency as responses. The optimized proniosomal gel was characterized by vesicle size, entrapment efficiency, transmission electron microscopy (TEM), in vitro drug release, skin retention studies, skin irritation studies and stability studies. The optimised batch showed vesicle size of 2.27±1.82 µ, and entrapment efficiency of 98.15±0.25 %. The optimised formulation was stable under refrigeration condition (5°C) in amber coloured bottle, was non-irritating and showed 98.10±1.28 % release and 85±1.53 % permeation after 6 h and 436±12 µg drug was retained in the skin after 3 hrs.

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