Implementing Central Composite Design for the Development of Tacrolimus Film for Sublingual Administration

MOHANAN, JISHA; Subramaniyan, Gopinath; KUTTALINGAM, ARUL; Damodharan, N

doi:10.22159/ijap.2023v15i3.47265

Cited by 2 publications

(1 citation statement)

References 23 publications

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“…The preparation and evaluation of tacrolimus-loaded fast-dissolving films and tablets had already been discussed in earlier publications by Mohanan J. and co-authors. 5,6 To brief, to enhance the solubility of the drug, firstly, inclusion complexes with β-cyclodextrin were developed and characterized followed by their formulation into fast-dissolving films and tablets for sublingual administration. The optimized formulations were further selected for their in vivo bioavailability study in rabbits.…”

Section: Development Of Tacrolimus Loaded Fast Dissolving Films and T...mentioning

confidence: 99%

Pharmacokinetic Exploration of Sublingual Route for the Enhanced Bioavailability of Tacrolimus with Rabbit as Animal Model

Mohanan,

Subramaniyan,

Kuttalingam

et al. 2023

Int J. Pharm. Investigation

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Introduction:The study aimed to assess the bioavailability of two sublingual formulations i.e., fast-dissolving films and tablets of the poorly bioavailable immunosuppressant drug, tacrolimus, and to compare with its marketed oral capsule formulation. Materials and Methods: Optimized film and tablet formulations of tacrolimus for sublingual administration were developed. Stability studies were performed at room temperature as well as at 40±2°C/75±2% relative humidity for 6 months. The in vivo pharmacokinetic studies were performed with rabbits as the animal model. Different pharmacokinetic parameters like t max, C max , AUC, t 1/2 and Ke were established and they were analyzed statistically by the student t-test. Results: The stability analysis showed a satisfactory stability profile of all the dosage forms in a six-month study. The in vivo study of the developed formulations showed better pharmacokinetic performance when compared with the marketed oral formulation. There was approximately a 2 and 1.8-fold increase in the relative bioavailability of the film and the tablet formulations respectively. Conclusion: The development of tacrolimus into sublingual dosage forms could improve the in vivo performance of the drug candidate.

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Section: Development Of Tacrolimus Loaded Fast Dissolving Films and T...mentioning

confidence: 99%

Pharmacokinetic Exploration of Sublingual Route for the Enhanced Bioavailability of Tacrolimus with Rabbit as Animal Model

Mohanan,

Subramaniyan,

Kuttalingam

et al. 2023

Int J. Pharm. Investigation

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The Choice of Components and the Impact of Surfactants and Co-Surfactants on Eplerenone Nanoemulsion Synthesis for Gel-Based Transdermal Application

GAIKWAD,

MARATHE,

PATHAN

2024

Int J App Pharm

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Objective: This research aims to establish an efficient methodology for selecting nanoemulsion components to synthesize eplerenone nanoemulsion for gel-based transdermal applications. Methods: The chemical compatibility study of eplerenone was investigated by FTIR, DSC, and solubility in oils, surfactants, and co-surfactants as the criteria for choice. We used visual appraisal and grading to assess the effectiveness of emulsification. Various excipients were tested depending on solubility. The final appearance, dispersibility, and ease of emulsification were used to visually assess the degree of self-emulsification of oil and emulsifier in a 1:3 mass ratio. Co-surfactants were assessed by mixing particular emulsifiers in a 2:1 (w/w) ratio with co-surfactants, and the oily component was added at a 1:3 (w/w) ratio to evaluate Smix's emulsification potential. A central composite design synthesized, evaluated, and optimized eplerenone nanoemulsions. Optimized nanoemulsions were characterized after a thermodynamic stability study for droplet size, ζ potential, viscosity, refractive index, pH measurements, and TEM. All the selected formulations were found to be stable, and the droplet size was found to be<110 nm. Results: Eplerenone was chemically compatible, and its maximum solubility was 171.3±0.92 and 169.3±2.22 in Kollicream®OA and Paceol, respectively. The evidence impressively found that Tween 20 and Kolliphor®EL were discovered as active emulsifiers, and Transcutol®P was revealed to be a co-surfactant. Outcomes showed that the emulsification efficacy of Kolliphor®EL (3% w/w) was able to emulsify Kollicream®OA (1% w/w), and Paceol failed. As well, Smix [Kolliphor®EL (2% w/w) and Transcutol®P (1% w/w)] were able to emulsify Kollicream®OA (1% w/w). Conclusion: The main conclusion from this work is the application of a visual appraisal and grading system to assess the final appearance, dispersibility, and ease of emulsification to eradicate the toxicity and irritation that nanoemulsions can cause. Optimised nanoemulsions can further formulate eplerenone's nanoemulsion gel for transdermal application.

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Implementing Central Composite Design for the Development of Tacrolimus Film for Sublingual Administration

Cited by 2 publications

References 23 publications

Pharmacokinetic Exploration of Sublingual Route for the Enhanced Bioavailability of Tacrolimus with Rabbit as Animal Model

Pharmacokinetic Exploration of Sublingual Route for the Enhanced Bioavailability of Tacrolimus with Rabbit as Animal Model

The Choice of Components and the Impact of Surfactants and Co-Surfactants on Eplerenone Nanoemulsion Synthesis for Gel-Based Transdermal Application

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