豚の耳と人間の前腕の毛包へのナノ粒子の取り込みの定量化

特にナノ粒子（NP）を使用した毛包（HF）を介した薬物送達は、デポ効果と下部HF内の吸収条件を促進したため、最近注目を集めました。経皮薬物送達の見通しにより、NPの卵胞の取り込みを最適化することは興味深い。この研究では、HFへのNPの取り込みを定量化する方法が開発され、豚の耳モデルとin vivoでin vitroで適用されました。HF取り込みに対するNP材料の影響は、ポリ（D、L-ラクタイド-Co-グリコリド）（PLGA）に基づく蛍光標識NPを使用して調査されました。すべてのNPには、同様の流体力学サイズ（163-170 nm）がありましたが、異なる表面修飾：（i）プレーンPLGA、（ii）キトサンコーティングPLGA（chit.-plga）、および（iii）異なるリン脂質でコーティングされた（iii）chit.-plga（PL）（DPPC（100）、DPPC：chol（85：15）、dPC：（92：8）は、蛍光の定量化のためにサンプルを抽出しました。in vitroモデルは、両方のモデル間で優れたin vitro-in vivo相関（2）= 0.987）を実証し、HFへのNPの摂取量を定量化するために、人間のin vivoの状況の代替性をさらにサポートします。

Drug delivery via the hair follicle (HF) especially with nanoparticles (NP) recently gained attention due to a depot effect and facilitated absorption conditions within the lower HF. With the prospect of transdermal drug delivery, it is of interest to optimize the follicular uptake of NP. In this study, a method was developed to quantify NP uptake into HF and applied in vitro in a pig ear model and in vivo in human volunteers. The influence of NP material on HF uptake was investigated using fluorescence-labeled NP based on poly(D,L-lactide-co-glycolide) (PLGA). All NP had similar hydrodynamic sizes (163-170 nm) but different surface modifications: (i) plain PLGA, (ii) chitosan-coated PLGA (Chit.-PLGA), and (iii) Chit.-PLGA coated with different phospholipids (PL) (DPPC (100), DPPC:Chol (85:15), and DPPC:DOTAP (92:8). Differential stripping was performed, including complete mass balance. The samples were extracted for fluorescence quantification. An effect of the PL coating on follicular uptake was observed as DPPC (100) and DPPC:DOTAP (92:8) penetrated into HF to a higher extent than the other tested NP. The effect was observed both in the pig ear model as well as in human volunteers, although it was statistically significant only in the in vitro model. An excellent in vitro-in vivo correlation (IVIVC, r(2)=0.987) between both models was demonstrated, further supporting the suitability of the pig ear model as a surrogate for the in vivo situation in humans for quantifying NP uptake into HF. These findings may help to optimize NP for targeting the HF and to improve transdermal delivery.