Scholarlink

<p>Psoriasis is a chronic inflammatory skin disease that is known to cause hyperproliferation of keratinocytes and the formation of erythematous scaly plaques. Although apremilast in the form of a phosphodiesterase-4 inhibitor is used to treat plaque psoriasis and psoriatic arthritis, it is known to produce systemic side effects and is less patient-compliant. The aim of the current study is to formulate and optimise the formulation of apremilast-loaded cubosomes suspensions in gel vehicles. This is to enhance the drug solubility, the permeability of the drug across the skin, and the sustained release of the drug. Apremilast-loaded cubosomes were formulated by a sonication method with a lipid phase composed of glycerol monooleate and a surfactant phase consisting of a stabilising agent, i.e., Poloxamer 407. The processing-related factors for apremilast-loaded cubosomes were optimised, considering a central composite design. The drug permeation behaviour revealed a sustained release pattern under in vitro studies. The optimised apremilast-loaded cubosomes have a particle size distribution, given as 53.95 ± 0.23&#xa0;nm, with a corresponding polydispersity index of 0.268 ± 0.021, to be appropriate for their topical application. The result namely, a significant increase in drug permeation, twice that achieved by a conventional apremilast-containing gel, was highlighted during in vivo studies. The cubosomal gel was further found to demonstrate excellent biocompatibility, as confirmed by skin irritation studies, providing a sense of comfort to patients, hence increasing compliance. The drug also reduced symptoms in imiquimod-induced psoriatic animal models. In summary, the newly formulated apremilast-containing cubosomal gel has the potential to circumvent the use of the orally administered drug by addressing the physicochemical constraints of apremilast from the viewpoint of solubility, permeability, and bioavailability. The absence of skin irritation in addition to its higher therapeutic effectiveness in an animal model further proves the worth of the formulated drug. It is recommended to further explore the translational study of the drug to test its applicability in real-world cases.</p> Graphical Abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Development and Optimization of Apremilast-Loaded Cubosomes for Enhanced Topical Delivery and Psoriasis Management

  • 期刊论文

  • 发表日期：

    2026年4月23日

查看全文
  • A. Akhila,
  • Marina Koland,
  • Suprit D. Saoji,
  • Ananya N. Devadiga,
  • S. M. Sindhoor,
  • Mohammad Adnan Raza

摘要

Psoriasis is a chronic inflammatory skin disease that is known to cause hyperproliferation of keratinocytes and the formation of erythematous scaly plaques. Although apremilast in the form of a phosphodiesterase-4 inhibitor is used to treat plaque psoriasis and psoriatic arthritis, it is known to produce systemic side effects and is less patient-compliant. The aim of the current study is to formulate and optimise the formulation of apremilast-loaded cubosomes suspensions in gel vehicles. This is to enhance the drug solubility, the permeability of the drug across the skin, and the sustained release of the drug. Apremilast-loaded cubosomes were formulated by a sonication method with a lipid phase composed of glycerol monooleate and a surfactant phase consisting of a stabilising agent, i.e., Poloxamer 407. The processing-related factors for apremilast-loaded cubosomes were optimised, considering a central composite design. The drug permeation behaviour revealed a sustained release pattern under in vitro studies. The optimised apremilast-loaded cubosomes have a particle size distribution, given as 53.95 ± 0.23 nm, with a corresponding polydispersity index of 0.268 ± 0.021, to be appropriate for their topical application. The result namely, a significant increase in drug permeation, twice that achieved by a conventional apremilast-containing gel, was highlighted during in vivo studies. The cubosomal gel was further found to demonstrate excellent biocompatibility, as confirmed by skin irritation studies, providing a sense of comfort to patients, hence increasing compliance. The drug also reduced symptoms in imiquimod-induced psoriatic animal models. In summary, the newly formulated apremilast-containing cubosomal gel has the potential to circumvent the use of the orally administered drug by addressing the physicochemical constraints of apremilast from the viewpoint of solubility, permeability, and bioavailability. The absence of skin irritation in addition to its higher therapeutic effectiveness in an animal model further proves the worth of the formulated drug. It is recommended to further explore the translational study of the drug to test its applicability in real-world cases.

Graphical Abstract