Benzyl Benzoate-Loaded Microemulsion for Topical Applications: Enhanced Dermatokinetic Profile and Better Delivery Promises.

Abstract

Benzyl benzoate (BB) is one of the oldest drugs used for the treatment of scabies and is recommended as the "first-line intervention" for the cost-effective treatment of the disease. Though a promising candidate, its application is reported to be associated with irritation of the skin and eye, resulting in poor patient compliance. Hence, the present study aims to develop BB-loaded topical microemulsion for the safer and effective delivery of BB. Pseudo-ternary phase diagrams with BB as the oily phase itself, along with Tween 80 as surfactant, and mixture of phospholipid and ethanol as the co-surfactant along with aqueous solution as the external phase were constructed and various compositions were formulated. The optimized formulation was characterized for particle-size, zeta-potential, drug-content, globule-morphology pH, and refractive-index, whereas evaluated for skin permeation, retention, compliance, and dermatokinetics. The nanosized formulation offered threefold higher drug permeation vis-a-vis plain drug solution across LACA mice abdominal skin. The drug retention of the selected formulation was nearly twice of that from the marketed product, assuring depot formulation and sustained release. The skin histopathology revealed the non-irritant nature of the formulation, as no changes in the normal skin histology were observed. The dermatokinetic studies confirmed better permeation and enhanced skin bioavailability of BB to epidermis as well as dermis vis-à-vis the conventional product. The results indicate that the developed lipid-based microemulsion hydrogel can alleviate the concerns associated with BB and can provide a better and safer delivery option in substantial amounts to various skin layers.

• Authors: Gajanand Sharma, Geeta Dhankar, Kanika Thakur, Kaisar Raza, O P Katare
• Journal: AAPS PharmSciTech (AAPS PharmSciTech) Vol. 17 Issue 5 Pg. 1221-31 (Oct 2016) ISSN: 1530-9932 [Electronic] United States
• PMID: 26669889 (Publication Type: Journal Article)

Chemical References

• Benzoates
• Drug Carriers
• Emulsions
• Polysorbates
• Surface-Active Agents
• Hydrogel, Polyethylene Glycol Dimethacrylate
• benzyl benzoate

Topics

• Administration, Topical
• Animals
• Benzoates (administration & dosage, chemistry, metabolism)
• Biological Availability
• Chemistry, Pharmaceutical (methods)
• Drug Carriers (chemistry)
• Drug Delivery Systems (methods)
• Drug Stability
• Emulsions (administration & dosage, chemistry, metabolism)
• Hydrogel, Polyethylene Glycol Dimethacrylate (chemistry)
• Male
• Mice
• Nanoparticles (administration & dosage, chemistry, metabolism)
• Particle Size
• Permeability
• Polysorbates (chemistry)
• Skin (metabolism)
• Skin Absorption
• Surface-Active Agents (chemistry)