Fabricating transdermal film formulations of montelukast sodium with improved chemical stability and extended drug release

Aashli,; Reddy, S. Giridhar; Belliraj, Siva Kumar; Prashanthi, K.; Murthy, H. C. Ananda

doi:10.1016/j.heliyon.2023.e14469

Cited by 8 publications

(5 citation statements)

References 29 publications

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“…Hydrogels have been used in drug delivery system over decades. Its capability to adsorb water with a controlled kinetics of dissolution render this material suitable for carrying and delivery of different bioactive molecules, conductive components and cell types 22,23 . To date, the combination of SA and P407 has been evaluated for diverse biomedical applications such as topic gels, 24–26 injectable hydrogels, 21 membranes 27 and foams 28 .…”

Section: Resultsmentioning

confidence: 99%

“…Its capability to adsorb water with a controlled kinetics of dissolution render this material suitable for carrying and delivery of different bioactive molecules, conductive components and cell types. 22,23 To date, the combination of SA and P407 has been evaluated for diverse biomedical applications such as topic gels, [24][25][26] injectable hydrogels, 21 membranes 27 and foams. 28 However, these studies usually involve further functionalities to the pristine materials which address some issues regarding the safety aspects.…”

Section: Protein Release Profilementioning

confidence: 99%

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Interpenetrating alginate network as drug delivery matrix: Effects on protein stability and release

Monteiro,

Pérez‐Jiménez,

Spitzlei

et al. 2023

J Biomed Mater Res

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The study investigates the rheological properties and protein release capacity of a uniform hydrogel composed of sodium alginate (SA) and poloxamer (P407). The hydrogel is prepared through the sustained release of calcium ions, resulting in a reinforced and homogeneous interpenetrating networks (IPNs) of SA and P407 polymeric chains. By adjusting the amount of crosslink agent, the hydrogel exhibites an adjustable dissolution ratio and adaptable gelling time. Moreover, the composite showed a well‐structured network and superior mechanical strength, enabling the sustained release of both calcium ions and Soybean Trypsin Inhibitor (STI) protein, a model of Bone Morphogenic Protein (BMP). Importantly, the protein release kinetic can be tuned based on the SA content in the polymeric blend, highlighting the versatile nature of this hydrogel for drug delivery purposes.

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Section: Resultsmentioning

confidence: 99%

Section: Protein Release Profilementioning

confidence: 99%

Interpenetrating alginate network as drug delivery matrix: Effects on protein stability and release

Monteiro,

Pérez‐Jiménez,

Spitzlei

et al. 2023

J Biomed Mater Res

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“…Retention times obtained were comparable to real samples with no interfering peaks. As MTS belongs to a BCS class II drug with a log P value of 8.49 [22,39], extraction of the drug from plasma needs to be done by a non-polar solvent. Among all tried non-polar solvents tetra-butyl-methyl-ether showed good recovery and zero interference with both drug and internal standard [22].…”

Section: Discussionmentioning

confidence: 99%

IVIVC assessment, pharmacokinetic evaluation, and X-ray radiography mapping of Novel Parteck® SRP 80 and hypromellose-loaded LTD4 receptor antagonist chronosystem

Jawed,

Satish

2023

Futur J Pharm Sci

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Background The current research aims to determine the pharmacokinetic parameters, mucoadhesive strength, and IVIVC correlation of the novel chronotherapeutic drug delivery system of montelukast sodium (MTS) loaded Parteck® SRP80 and hypromellose system. To accomplish this, an HPLC method was developed which is highly sensitive, precise, and rapid for quantifying pure MTS in rabbit plasma. Mucoadhesive strength and time-dependent mobility of developed formulation were established by ex-vivo study and X-ray radiography, respectively. Using a fraction of drug absorbed (FDA) and a fraction of drug released (FDR), Level-A in-vitro in-vivo correlation (IVIVC) was developed. According to ICH Q1A (R2) standards, stability experiments were conducted for 180 days. Result MTS retention time came as 3.971 min with a mobile phase of methanol: acetonitrile: 0.2 mM sodium acetate buffer (5:90:5). In-vitro dissolution showed pulsatile release of the drug up to 24 h with two lag phases. The in-vivo study showed a Cmax of 490.16 ± 33.95 ng/ml, Tmax of 9 h, and MRT of 14.08 ± 1.21 h. The correlation coefficient of 0.9899 confirmed the level-A IVIVC. Uncoated matrix tablet of Parteck® SRP 80 displayed mucoadhesive strength 1.25-fold higher than hypromellose. Stability experiments found no significant changes in drug content, physical appearance, and cumulative percentage release with a similarity factor of 87–90. Conclusion A single oral dose in-vivo study proved the sustained release of the drug for 24 h with satisfactory mucoadhesive strength. Moreover, X-ray radiography has confirmed the time-dependent presence of formulation at the needed spot. This study fulfilled all the requirements for chronotherapy of asthma and can be scaled up in the future. Graphical abstract

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“…The thermogram of montelukast sodium and montelukast sodium mixed with lactose monohydrate or croscarmellose sodium is shown in Figure 4(b). From the literature, the melting point of montelukast sodium is varied including 275.9 F (=135.5 °C) (Reddy et al, 2023), 138.6-139.8 °C (Hadi et al, 2012Shruthi and Thahera, 2013). However, the DSC thermogram result showed that the melting point of montelukast in this study is 154 °C (see Figure 4b).…”

Section: Montelukast Sodium Granules Characteristicsmentioning

confidence: 99%

Development of Pharmaceutical Equivalent Montelukast Sodium Immediate-Release, Film-Coated Tablets

Muenraya,

Atipairin,

Srichana

et al. 2024

Sci. Technol. Indones

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Montelukast tablets are sold under the brand name Singulair and are used to control and prevent asthma symptoms. In this study, 10 mg film-coated montelukast tablets were developed as a generic drug in order to evaluate the pharmaceutical equivalent of the innovator’s products. The primary formulation ingredients used in all developed formulations (F1-F5) were the same as those described in the Singulair tablet package insert, except for formulations F3, F4, and F5, to which solubilizing enhancers were added to increase montelukast solubility. The core tablets were produced using the wet granulation method before being coated with HPMC polymer. FT-IR and DSC were used to determine drug and excipient compatibility. The micromeritic properties of the granules were assessed. The physicochemical properties of generated montelukast tablets and Singulair tablets were also investigated. The dissolution profiles of the tested drug and the innovator were assessed in a variety of pH mediums (pH 1.2, 4.5, 6.8, and water). The similarity (f2) and difference (f1) factors were computed. The accelerated and long-term stability of the tested drug in hot and humid climate zones was evaluated. The analytical method validation used in this study was ICH-acceptable for 8 parameters including specificity, range, linearity, accuracy, precision, limit of detection, limit of quantitation, and robustness. F1-F5 granules had similar properties, such as a pale-yellow color and excellent flow properties. There were no chemical interactions between montelukast and the excipients according to FT-IR and DSC analyses. The physical properties of all developed montelukast film-coated tablets were similar (average weight 212-218 mg; thickness 3.02-3.07 mm; assay 101-102% LA; disintegration time 3-4 min), except that the disintegration time of F3 was 8.10 min and that of F5 was 5.90 min, which was caused by the addition of poloxamer 188 to the formulation. In all mediums, only the F1 formula produced acceptable comparison dissolution profiles to Singulair. After 6 months of storage under accelerated and long-term conditions, the results showed the F1 formulation remained physically and chemically stable.

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Fabricating transdermal film formulations of montelukast sodium with improved chemical stability and extended drug release

Cited by 8 publications

References 29 publications

Interpenetrating alginate network as drug delivery matrix: Effects on protein stability and release

Interpenetrating alginate network as drug delivery matrix: Effects on protein stability and release

IVIVC assessment, pharmacokinetic evaluation, and X-ray radiography mapping of Novel Parteck® SRP 80 and hypromellose-loaded LTD4 receptor antagonist chronosystem

Development of Pharmaceutical Equivalent Montelukast Sodium Immediate-Release, Film-Coated Tablets

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