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CHI TIẾT
Nghiên cứu xây dựng công thức bào chế emugel alpha arbutin 1% (Phần 1)
Study on formulation of alpha arbutine emulgel 1% (Part 1)
Trần Thị Hải Yến, Khil Kosol, Lê Thị Thu Trang, Vũ Thị Thu Giang
Số: 526 - Tháng 2/2020 - Trang 52-55

Rối loạn tăng sắc tố da (nám, tàn nhang, đốm lão hóa,…) là hiện tượng phổ biến, tuy không ảnh hưởng đến sức khỏe con người nhưng tác động rất nhiều về mặt tâm lý. Có rất nhiều phương pháp cải thiện tình trạng này, chủ yếu được chia thành hai nhóm: nhóm các tác nhân hóa học (hydroquinon, arbutin, alpha arbutin, acid kojic, acid ascorbic và các dẫn xuất…) và nhóm các phương thức trị liệu vật lý (liệu pháp lạnh với nitơ lỏng, phẫu thuật laser…). Trong số các phương thức trên, can thiệp bằng các tác nhân hóa học vẫn giữ vai trò chủ chốt trong điều trị các rối loạn tăng sắc tố da cũng như ứng dụng trong lĩnh vực mỹ phẩm để làm trắng da. Trước đây, hydroquinon là một chất làm trắng da nhanh nhất và hiệu quả nhất, được ứng dụng rộng rãi trong điều trị tăng sắc tố da. Nhưng cho đến thời điểm hiện tại hydroquinon đã bị cấm sử dụng trên da do có nhiều tác dụng không mong muốn. Hiện nay alpha-arbutin là một chất an toàn và ổn định hơn so với hydroquinon, được sử dụng trong các chế phẩm mỹ phẩm làm trắng da và toàn thân. Để có tác dụng điều trị trên da, alpha-arbutin cần thấm qua lớp sừng. Trong khi đó, emulgel là dạng bào chế có cấu trúc nhũ tương, trong đó pha dầu được phân tán trong pha ngoại có chứa chất tạo gel. Do đó, emulgel ngoài ưu điểm làm tăng thấm dược chất qua lớp sừng, nó còn bền vững hơn so với kem thông thường do độ nhớt của pha ngoại lớn nhờ có tá dược tạo gel. Ngoài ra, emulgel có tỉ lệ pha dầu ít hơn dạng kem nên hạn chế tác dụng gây trơn nhờn da, phù hợp với chế phẩm mỹ phẩm. Do vậy nghiên cứu tiến hành với mục tiêu xây dựng công thức bào chế emulgel chứa alpha – arbutin.

Nguyên liệu: Alpha – arbutin có xuất xứ Mỹ. Alcol cetylic, vaselin, Tween 80, Span 80, glycerin, isopropyl myristat, Nipagin, Nipasol, polyvinyl pyrolidon K30 (PVPk30), carboxymethyl cellulose (CMC), hydroxypropyl methyl cellulose K100M (HPMC K100M) có xuất xứ Trung Quốc. Carbopol 934 có xuất xứ Đức. Methanol sắc ký được mua từ công ty J. T. Baker (Mỹ). Nước cất được điều chế tại phòng thí nghiệm Việt Nam.

- Thiết bị: Máy khuấy chân vịt Wisestir HS-120A (Đức); Hệ thống sắc ký lỏng hiệu năng cao Agilent (Mỹ); thiết bị phân tích kích thước Zetasizer nano ZS90 (Malvern – Anh); Cân phân tích Satorius BP121S (Đức), máy đo pH Mettler Toledo (Đức); bể siêu âm Ultrasonic LC 60H (Đức); thiết bị ly tâm Hermle Z 200 A (Đức).

Phương pháp nghiên cứu

- Phương pháp bào chế emulgel chứa alpha-arbutin 1 %.

- Phương pháp đánh giá emulgel arbutin.

            Kết luận

Đã xây dựng được công thức bào chế emugel alpha arbutin, trong đó sử dụng tỉ lệ các thành phần pha dầu thấp, sử dụng carbopol để tạo gel, điều chỉnh thể chất cho pha nước. Hệ đệm citro-phosphat pH 5,0-6,5 cho emulgel đồng nhất, ổn định về trạng thái phân tán, kích thước trung bình của các giọt dầu đạt khoảng 180 nm, PDI nhỏ hơn 0,3.

In view that alpha-arbutin is a safe substance used in whitening cosmeceutical preparations for therapy of hyperpigmentation disorders, and on the other hand, emulgel fomulations are favouurable preparations for that in emulsion structure they are much advantagous over the conventional creams in various aspects, such as increasing permeability of active ingredients through the stratum corneum, imprving physical stability, and lowering oil contents,… alpha-arbutin emulgel 1% was formulated, prepared by by emulsification and the obtained emulgel preparations were characterized. The particle size of the oil drops was evaluated by dynamic light scattering, and alpha-arbutin contents were determined by HPLC. The use of carbopol 934 as gel-forming excipient and triethanolamin as neutralizer in aqueous phase rendered good appearance and high physical stability to the formulated emulgels. Emulgels with pH 5.0-6.5 took elegant appearance, the average particle size of the oil drops ranged at about 180 nm, PDI was less than 0.3.

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