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<p>Bromocriptine mesylate (BCM) on oral administration shows low bioavailability due to limited gastric absorption (30%) and is susceptive to substantial first pass metabolism in the liver. Bromocriptine is classified under Biopharmaceutics Classification System (BCS) as a Class II drug (low solubility, high permeability), which rationalizes the need for an alternative route to bypass dissolution-limited absorption and first-pass metabolism. It shows a biological half-life 2 to 6&#xa0;h. It is used as a dopaminergic agonist indicated for Parkinson’s disease (PD). This study aims to develop, characterize and statistically optimize a BCM entrapped ultra-flexible deformable liposome (UDL) loaded into a gel formulation to study its efficacy in transdermal penetration and thereby improve its pharmacokinetic profile. Impact of different formulation factors on crucial qualities including entrapment efficiency was analyzed using a full factorial design. Hydration of deposited thin film was done to develop BCM entrapped UDL. The Optimized formulation shown zeta potential value (–) 13.0 mV and mean vesicle size of UDL was found to be 148.5&#xa0;nm. In an ex-vivo diffusion study, UDL showed a significant increase in transdermal penetration across isolated rat skin was observed as compared to an aqueous BCM solution. In the in-vivo pharmacokinetic studies in Wistar rats showed a higher and prolonged drug release from UDL loaded gel formulation as compared to oral, intravenous aqueous BCM solution and BCM impregnated DIA transdermal patch. In the in-vivo pharmacokinetic studies AUC0–t for developed formulation, oral, intravenous BCM solution and BCM in adhesive based transdermal patch was found to be 30979.83, 7705.75, 20282.58 and 14753.51 ng/ml h respectively. The results of studies suggest that the BCM entrapped UDL loaded gel might be a preferable and patient compliant alternative than oral administration of BCM for management of Parkinson’s disease.</p>

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Ultra-Flexible Liposomal Gels Versus Pressure-Sensitive Adhesive Transdermal Patches: A Comparative Pharmacokinetic Study for Effective Management of Parkinson’s Disease

  • 期刊论文

  • 发表日期：

    2025年11月25日

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  • Afridi Chabru,
  • Pramod Salve,
  • Mohammad Qutub,
  • Ujban Hussain,
  • Amol Tatode,
  • Samiksha Tammewar,
  • Sameer Sheikh,
  • Tanvi Premchandani

摘要

Bromocriptine mesylate (BCM) on oral administration shows low bioavailability due to limited gastric absorption (30%) and is susceptive to substantial first pass metabolism in the liver. Bromocriptine is classified under Biopharmaceutics Classification System (BCS) as a Class II drug (low solubility, high permeability), which rationalizes the need for an alternative route to bypass dissolution-limited absorption and first-pass metabolism. It shows a biological half-life 2 to 6 h. It is used as a dopaminergic agonist indicated for Parkinson’s disease (PD). This study aims to develop, characterize and statistically optimize a BCM entrapped ultra-flexible deformable liposome (UDL) loaded into a gel formulation to study its efficacy in transdermal penetration and thereby improve its pharmacokinetic profile. Impact of different formulation factors on crucial qualities including entrapment efficiency was analyzed using a full factorial design. Hydration of deposited thin film was done to develop BCM entrapped UDL. The Optimized formulation shown zeta potential value (–) 13.0 mV and mean vesicle size of UDL was found to be 148.5 nm. In an ex-vivo diffusion study, UDL showed a significant increase in transdermal penetration across isolated rat skin was observed as compared to an aqueous BCM solution. In the in-vivo pharmacokinetic studies in Wistar rats showed a higher and prolonged drug release from UDL loaded gel formulation as compared to oral, intravenous aqueous BCM solution and BCM impregnated DIA transdermal patch. In the in-vivo pharmacokinetic studies AUC0–t for developed formulation, oral, intravenous BCM solution and BCM in adhesive based transdermal patch was found to be 30979.83, 7705.75, 20282.58 and 14753.51 ng/ml h respectively. The results of studies suggest that the BCM entrapped UDL loaded gel might be a preferable and patient compliant alternative than oral administration of BCM for management of Parkinson’s disease.