Abstract

Objective: The objective of this present work was to develop the chemical peeling cream containing the synthesized active ingredient pharmaceutical cocrystal of salicylic acid and phenylalanine.
 Methods: The salicylic acid and phenylalanine cocrystal (H2Sal·Phe) was synthesized by the solvent evaporation method and characterized by various techniques such as single-crystal X-ray diffraction and Fourier transform infrared spectroscopy. The five formulas of cocrystal cream were prepared. All formulas were then examined and observed for appearance, spreadability, viscosity, pH, homogeneity, SPF test, microbial limit test and stability test.
 Results: The (H2Sal·Phe) consists of no zwitterion phenylalanine for the first time. X-ray crystal structure of cocrystal consists of double H2Sal and Phe molecules with stabilized by inter-, intra-molecular and π-π interactions. By using this cocrystal as an active ingredient for cosmetic development, the chemical peeling cream was produced along with the pharmaceutical examinations. The (H2Sal·Phe) formulations were prepared 0-1% and excipients included of jojoba oil, isopropyl myristate, castor oil, glyceryl monostearate cetostearyl alcohol, cyclomethicone (and) dimethicone crosspolymer, vitamin E, white bee's wax, glycerin, PEG 400, xanthan gum, Span 80 and Tween 60. We finally found that the F4 (1% H2Sal·Phe) was the best formulation with suitable physical properties of cream and chemical stable after storage. The results of cell viability show H2Sal·Phe is non-toxic with cell.
 Conclusion: The chemical peeling cream containing (H2Sal·Phe) has shown the promising results which are both safe and efficacious peeling agent. Cocrystal (H2Sal·Phe) cream can be used as an alternative choice in whitening skin.

Highlights

  • Salicylic acid (H2Sal) is a beta-hydroxy acid and nonsteroidal anti-inflammatory drug (NSAID) [1,2,3]

  • Phenylalanine is an essential amino acid which is a building block for proteins in the body [6]. It may be used in cosmetics as well as personal care products, such as topical cream which use to help turn over the pigment-forming melanocytes which are essential in the initiation of pigmentation [1, 6,7,8]

  • It is known as salicylic acid chemical peels, alpha hydroxy acid (AHA) chemical peels, or glycolic acid peels which is the application of a chemical agent to the skin [7, 8]

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Summary

Introduction

Salicylic acid (H2Sal) is a beta-hydroxy acid and nonsteroidal anti-inflammatory drug (NSAID) [1,2,3]. It is a hydroxyl derivative of benzoic acid and represents a carboxylic acid attached to aromatic alcohol, phenol [1]. It is known as skin disorder treatments such as keratolytic properties because of the solubility of intracellular cement. Cocrystals are generally formed through noncovalent interaction bonds (primarily hydrogen bonding), π–π stacking, van der Waals interactions and other weak interactions [10,11,12]

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