Transdermal delivery of gatifloxacin carboxymethyl cellulose-based patches: Preparation and characterization

Ullah, Wasi; Nawaz, Asif; Akhlaq, Muhammad; Shah, Kifayat Ullah; Latif, Muhammad Shahid; Doolaanea, Abd Almonem; Alfatama, Mulham

doi:10.1016/j.jddst.2021.102783

Cited by 13 publications

(17 citation statements)

References 32 publications

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“…Thickness of the formulated transdermal patches was evaluated using a vernier caliper (Ossenpaß 4, 47623 Kevelaer, Germany, +49-2832-92390). At six different places, the thickness of the formulated transdermal patches was measured, and the results were calculated and averaged [ 19 ].…”

Section: Methodsmentioning

confidence: 99%

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Formulation and Evaluation of Hydrophilic Polymer Based Methotrexate Patches: In Vitro and In Vivo Characterization

et al. 2022

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This study attempted to develop and evaluate controlled-release matrix-type transdermal patches with different ratios of hydrophilic polymers (sodium carboxymethylcellulose and hydroxypropyl methylcellulose) for the local delivery of methotrexate. Transdermal patches were formulated by employing a solvent casting technique using blends of sodium carboxymethylcellulose (CMC-Na) and hydroxypropylmethylcellulose (HPMC) polymers as rate-controlling agents. The F1 formulated patch served as the control formulation with a 1:1 polymer concentration. The F9 formulation served as our optimized formulation due to suitable physicochemical properties yielded through the combination of CMC-Na and HPMC (5:1). Drug excipient compatibilities (ATR-FTIR) were performed as a preformulation study. The ATR-FTIR study depicted great compatibility between the drug and the polymers. Physicochemical parameters, kinetic modeling, in vitro drug release, ex vivo drug permeation, skin drug retention, and in vivo studies were also carried out for the formulated patches. The formulated patches exhibited a clear, smooth, elastic nature with good weight uniformity, % moisture uptake, drug content, and thickness. Physicochemical characterization revealed folding endurance ranging from 62 ± 2.21 to 78 ± 1.54, tensile strength from 9.42 ± 0.52 to 12.32 ± 0.72, % swelling index from 37.16 ± 0.17 to 76.24 ± 1.37, and % drug content from 93.57 ± 5.34 to 98.19 ± 1.56. An increase in the concentration of the CMC-Na polymer (F9) resulted in increased drug release from the formulated transdermal patches. Similarly, drug permeation and retention were found to be higher in the F9 formulation compared to the other formulations (F1–F8). A drug retention analysis revealed that the F9 formulation exhibited 13.43% drug retention in the deep layers of the skin compared to other formulations (F1–F8). The stability study indicated that, during the study period of 60 days, no significant changes in the drug content and physical characteristics were found. ATR-FTIR analysis of rabbit skin samples treated with the formulated transdermal patches revealed that hydrophilic polymers mainly affect the skin proteins (ceramide and keratins). A pharmacokinetic profile revealed Cmax was 1.77.38 ng/mL, Tmax was 12 h, and t1/2 was 17.3 ± 2.21. In vivo studies showed that the skin drug retention of F9 was higher compared to the drug solution. These findings reinforce that methotrexate-based patches can possibly be used for the management of psoriasis. This study can reasonably conclude that methotrexate transdermal matrix-type patches with CMC-Na and HPMC polymers at different concentrations effectively sustain drug release with prime permeation profiles and better bioavailability. Therefore, these formulated patches can be employed for the potential management of topical diseases, such as psoriasis.

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Section: Methodsmentioning

confidence: 99%

“…The formulated patches were folded constantly at the same place until a crack or break appeared. The folding of patches at the same place provided the value for folding endurance [ 19 ].…”

Section: Methodsmentioning

confidence: 99%

Formulation and Evaluation of Hydrophilic Polymer Based Methotrexate Patches: In Vitro and In Vivo Characterization

et al. 2022

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“…The folding endurance value is important during the formulation of transdermal patches. This test indicates that formulated patches can integrate with skin folding and do not break during use [24]. The drug release pattern of transdermal matrix-type patches can be affected by moisture uptake and moisture loss.…”

Section: Discussionmentioning

confidence: 82%

“…An analytical weighing balance (Shimadzu AX 200, Kyoto, Japan) was used for the determination of weight. Individual weight was compared with average weight [24].…”

Section: Weight Uniformitymentioning

confidence: 99%

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Ethyl Cellulose and Hydroxypropyl Methyl Cellulose Blended Methotrexate-Loaded Transdermal Patches: In Vitro and Ex Vivo

et al. 2021

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Transdermal drug delivery systems (TDDSs) have become innovative, fascinating drug delivery methods intended for skin application to achieve systemic effects. TDDSs overcome the drawbacks associated with oral and parenteral routes of drug administration. The current investigation aimed to design, evaluate and optimize methotrexate (MTX)-loaded transdermal-type patches having ethyl cellulose (EC) and hydroxypropyl methyl cellulose (HPMC) at different concentrations for the local management of psoriasis. In vitro release and ex vivo permeation studies were carried out for the formulated patches. Various formulations (F1–F9) were developed using different concentrations of HPMC and EC. The F1 formulation having a 1:1 polymer concentration ratio served as the control formulation. ATR–FTIR analysis was performed to study drug–polymer interactions, and it was found that the drug and polymers were compatible with each other. The formulated patches were further investigated for their physicochemical parameters, in vitro release and ex vivo diffusion characteristics. Different parameters, such as surface pH, physical appearance, thickness, weight uniformity, percent moisture absorption, percent moisture loss, folding endurance, skin irritation, stability and drug content uniformity, were studied. From the hydrophilic mixture, it was observed that viscosity has a direct influence on drug release. Among all formulated patches, the F5 formulation exhibited 82.71% drug release in a sustained-release fashion and followed an anomalous non-Fickian diffusion. The permeation data of the F5 formulation exhibited about a 36.55% cumulative amount of percent drug permeated. The skin showed high retention for the F5 formulation (15.1%). The stability study indicated that all prepared formulations had very good stability for a period of 180 days. Therefore, it was concluded from the present study that methotrexate-loaded transdermal patches with EC and HPMC as polymers at different concentrations suit TDDSs ideally and improve patient compliance for the local management of psoriasis.

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Synthesis and Formulation Design of Sideroxylon Mascatense Branches Extract Mediated Nano-Emulsion Cream: Characterization, Antimicrobial, Wound Healing and Antidiabetic Activities Assessment

Hayat,

Nawaz,

Ullah

et al. 2024

Waste Biomass Valor

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Transdermal delivery of gatifloxacin carboxymethyl cellulose-based patches: Preparation and characterization

Cited by 13 publications

References 32 publications

Formulation and Evaluation of Hydrophilic Polymer Based Methotrexate Patches: In Vitro and In Vivo Characterization

Formulation and Evaluation of Hydrophilic Polymer Based Methotrexate Patches: In Vitro and In Vivo Characterization

Ethyl Cellulose and Hydroxypropyl Methyl Cellulose Blended Methotrexate-Loaded Transdermal Patches: In Vitro and Ex Vivo

Synthesis and Formulation Design of Sideroxylon Mascatense Branches Extract Mediated Nano-Emulsion Cream: Characterization, Antimicrobial, Wound Healing and Antidiabetic Activities Assessment

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