Current Challenges and Future of Lipid Nanoparticles Formulations for Topical Drug Application to Oral Mucosa, Skin, and Eye

Author(s)

Guilherme, Viviane A. ^[1] ; Ribeiro, Ligia N. M. ^[1] ; Tofoli, Giovana Radomille ^[2] ; Franz-Montan, Michelle ^[3] ; de Paula, Eneida ^[1] ; de Jesus, Marcelo Bispo ^[1]

Affiliation

^[1] Univ Campinas UNICAMP, Inst Biol, Dept Biochem & Tissue Biol, Rua Monteiro Lobato 255, BR-13083862 Campinas, SP - Brazil

^[2] Sao Leopoldo Mand Inst & Res Ctr, Lab Inflammat, Rua Jose Rocha Junqueira 13, BR-1304575 Campinas, SP - Brazil

^[3] Univ Campinas UNICAMP, Piracicaba Dent Sch, Dept Physiol Sci, Piracicaba, SP - Brazil

• Document type: Review article
• Source: CURRENT PHARMACEUTICAL DESIGN; v. 23, n. 43, p. 6659-6675, 2017.
• Web of Science Citations: 5

Abstract

Background: Topical drug administration offers an attractive route with minimal invasiveness. It also avoids limitations of intravenous administration such as the first pass metabolism and presystemic elimination within the gastrointestinal tract. Furthermore, topical drug administration is safe, have few side effects, is easy to apply, and offers a fast onset of action. However, the development of effective topical formulations still represents a challenge for the desired effect to be reached, locally or systemically. Solid lipid nanoparticles and nanostructured lipid carriers are particular candidates to overcome the problem of topical drug administration. The nanometric particle size of lipid nanoparticles favors the physical adhesion to the skin or mucosal, what can also be attained with the formation of hybrid (nanoparticles/polymer) systems. Methods: In this review, we discuss the major challenges for lipid nanoparticles formulations for topical application to oral mucosa, skin, and eye, highlighting the strategies to improve the performance of lipid nanoparticles for topical applications. Next, we critically analyzed the in vitro and in vivo approaches used to evaluate lipid nanoparticles performance and toxicity. Conclusion: We addressed some major drawbacks related to lipid nanoparticle topical formulations and concluded the key points that have to be overcome to help them to reach the market in topical formulations to oral mucosa, skin, and eye. (AU)

• FAPESP's process: 14/03002-7 - Internalization and intracellular trafficking of nanoparticles: biological activity and nanotoxicological profile
• Grantee: Marcelo Bispo de Jesus
• Support Opportunities: Research Grants - Young Investigators Grants
• FAPESP's process: 14/14457-5 - Lipid-based nanocarriers (SLN/NLC and remote-loading liposomes) used to improve the upload and potency of local anesthetics
• Grantee: Eneida de Paula
• Support Opportunities: Research Projects - Thematic Grants