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Review
. 2022 Dec 15;14(12):2818.
doi: 10.3390/pharmaceutics14122818.

Improved Topical Drug Delivery: Role of Permeation Enhancers and Advanced Approaches

Victor Hmingthansanga  1 , Nidhi Singh  1 , Superna Banerjee  1 , Sivakumar Manickam  2 , Ravichandiran Velayutham  3 , Subramanian Natesan  1
Affiliations
Review

Improved Topical Drug Delivery: Role of Permeation Enhancers and Advanced Approaches

Victor Hmingthansanga et al. Pharmaceutics. .

Abstract

The delivery of drugs via transdermal routes is an attractive approach due to ease of administration, bypassing of the first-pass metabolism, and the large skin surface area. However, a major drawback is an inability to surmount the skin's stratum corneum (SC) layer. Therefore, techniques reversibly modifying the stratum corneum have been a classical approach. Surmounting the significant barrier properties of the skin in a well-organised, momentary, and harmless approach is still challenging. Chemical permeation enhancers (CPEs) with higher activity are associated with certain side effects restricting their advancement in transdermal drug delivery. Furthermore, complexity in the interaction of CPEs with the skin has led to difficulty in elucidating the mechanism of action. Nevertheless, CPEs-aided transdermal drug delivery will accomplish its full potential due to advancements in analytical techniques, synthetic chemistry, and combinatorial studies. This review focused on techniques such as drug-vehicle interaction, vesicles and their analogues, and novel CPEs such as lipid synthesis inhibitors (LSIs), cell-penetrating peptides (CPPs), and ionic liquids (ILs). In addition, different types of microneedles, including 3D-printed microneedles, have been focused on in this review.

Keywords: cell penetration peptides; drug delivery; ionic liquids; microneedle; permeation enhancers; stratum corneum; transdermal.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Microscopic structure of the skin.
Figure 2
Figure 2
Schematic representation of the epidermis layer.
Figure 3
Figure 3
Schematic representation of the permeation process through the skin.
Figure 4
Figure 4
Permeation process through the skin via drug–vehicle interaction.
Figure 5
Figure 5
Structure of ethosome, liposome, transferosome, and niosome.
Figure 6
Figure 6
(A) Various types of chemical permeation enhancers used in TDDSs and (B) 2D-chemical structures.
Figure 7
Figure 7
Mechanism of action of LSIs.
Figure 8
Figure 8
Formation of ILs and the effect on the skin barrier.
Figure 9
Figure 9
Microneedle approaches: (A) solid microneedles, (B) coated microneedles, (C) dissolving microneedles, (D) hollow microneedles, and (E) hydrogel microneedles.
Figure 10
Figure 10
The 3D-printed microneedles for transdermal drug delivery.
See this image and copyright information in PMC

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