Chế tạo Microneedles Tan Đầu Ngón Cho Giao Thoa Thuốc Meloxicam Qua Da

AAPS PharmSciTech - Tập 19 - Trang 1141-1151 - 2017
Jianmin Chen1,2, Weiyue Huang1, Ziyao Huang1, Shiqi Liu1, Yaling Ye1, Qinglian Li1, Meiping Huang1
1School of Pharmacy and Medical Technology, Putian University, Fujian, China
2Key Laboratory of Pharmaceutical Analysis and Laboratory Medicine (Putian University), Fujian Province University, Fujian, China

Tóm tắt

Microneedles tan (MNs) cung cấp một phương pháp đơn giản, ít xâm lấn để đưa meloxicam (MX) vào da. Tuy nhiên, việc chế tạo MNs tan vẫn gặp phải một số thách thức như thời gian sản xuất dài, mất hoạt tính thuốc và khó khăn trong việc điều chỉnh lượng thuốc nạp vào MN. Để giải quyết những vấn đề này, chúng tôi đã phát triển microneedles tan đầu (TD MNs). Nhiều loại thuốc đã được bọc thành công, và lượng MX dao động từ 37,23 ± 8,40 đến 332,53 ± 13,37 μg được kiểm soát chính xác. Các ảnh hưởng của quy trình chế tạo đến tính ổn định của biomacromolecule đã được nghiên cứu và nhận thấy rằng tyrosinase giữ được 90,4% hoạt tính trong quá trình chế tạo. Toàn bộ quy trình chế tạo MN chỉ mất khoảng 1 giờ. Để đánh giá thêm tiềm năng của TD MNs, TD MNs MX đã được chuẩn bị cho các thí nghiệm giải phóng in vitro, thí nghiệm giải phóng in vivo, đánh giá độ an toàn, nghiên cứu dược động học và nghiên cứu dược lực học. Kết quả cho thấy TD MNs MX mang lại một số ưu điểm như giải phóng nhanh chóng thuốc được bọc (91,72% trong 30 phút), phân phối thuốc hiệu quả đến da (79,18%), không gây kích ứng da rõ rệt, khả năng sinh khả dụng tương đối tốt (122,3%) và có những tác động chống viêm và giảm đau mạnh mẽ. Dựa trên kết quả này, chúng tôi tin rằng TD MNs có tiềm năng hứa hẹn cho việc giao thoa thuốc MX qua da.

Từ khóa

#microneedles; meloxicam; chế tạo; giao thoa thuốc; giảm đau; chống viêm

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