Polymethacrylate microparticles gel for topical drug delivery.
OBJECTIVE
Evaluating the potentials of particulate delivery systems in topical drug delivery.


METHODS
Polymethacrylate microparticles (MPs) incorporating verapamil hydrochloride (VRP) as a model hydrophilic drug with potential topical clinical uses, using Eudragit RS100 and Eudragit L100 were prepared for the formulation of a composite topical gel. The effect of initial drug loading, polymer composition, particularly the proportion of Eudragit L100 as an interacting polymer component and the HLB of the dispersing agent on MPs characteristics was investigated. A test MPs formulation was incorporated in gel and evaluated for drug release and human skin permeation.


RESULTS
MPs showed high % incorporation efficiency and % yield. Composition of the hybrid polymer matrix was a main determinant of MPs characteristics, particularly drug release. Factors known to influence drug release such as MPs size and high drug solubility were outweighed by strong VRP-Eudragit L100 interaction. The developed MPs gel showed controlled VRP release and reduced skin retention compared to a free drug gel.


CONCLUSIONS
Topical drug delivery and skin retention could be modulated using particulate delivery systems. From a practical standpoint, the VRP gel developed may offer advantage in a range of dermatological conditions, in response to the growing off-label topical use of VRP.
Labouta
Hagar Ibrahim
HI
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt. hagar80im@gmail.com
El-Khordagui
Labiba K
LK
D000180:Acrylic Resins / Q000737:chemistry*; D000287:Administration, Topical; D000328:Adult; D002121:Calcium Channel Blockers / Q000008:administration & dosage*; D002152:Calorimetry, Differential Scanning; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D005782:Gels; D006801:Humans; D066298:In Vitro Techniques; D008855:Microscopy, Electron, Scanning; D008875:Middle Aged; D010316:Particle Size; D011109:Polymethacrylic Acids / Q000737:chemistry*; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption / Q000187:drug effects; D012995:Solubility; D013499:Surface Properties; D014700:Verapamil / Q000008:administration & dosage*
D000180:Acrylic Resins; D002121:Calcium Channel Blockers; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005782:Gels; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; C050528:Eudragit RS; D014700:Verapamil