Skin permeating nanogel for the cutaneous co-delivery of two anti-inflammatory drugs

Abstract

The aim of this study was to develop an effective drug delivery system for the simultaneous topical delivery of two anti-inflammatory drugs, spantide II (SP) and ketoprofen (KP). To achieve this primary goal we have developed a skin permeating nanogel system (SPN) containing surface modified polymeric bilayered nanoparticles along with a gelling agent. Poly-(lactide-co-glycolic acid) and chitosan were used to prepare bilayered nanoparticles (NPS) and the surface was modified with oleic acid (NPSO). Hydroxypropyl methyl cellulose (HPMC) and Carbopol with the desired viscosity were utilized to prepare the nanogels. The nanogel system was further investigated for in vitro skin permeation, drug release and stability studies. Allergic contact dermatitis (ACD) and psoriatic plaque like model were used to assess the effectiveness of SPN. Dispersion of NPSO in HPMC (SPN) produced a stable and uniform dispersion. In vitro permeation studies revealed increase in deposition of SP for the SP-SPN or SP+KP-SPN in the epidermis and dermis by 8.5 and 9.5 folds, respectively than SP-gel. Further, the deposition of KP for KP-SPN or SP+KP-SPN in epidermis and dermis was 9.75 and 11.55 folds higher, respectively than KP-gel. Similarly the amount of KP permeated for KP-SPN or SP+KP-SPN was increased by 9.92 folds than KP-gel. The ear thickness in ACD model and the expression of IL-17 and IL-23; PASI score and TEWL values in psoriatic plaque like model were significantly less (p<0.001) for SPN compared to control gel. Our results suggest that SP+KP-SPN have significant potential for the percutaneous delivery of SP and KP to the deeper skin layers for treatment of various skin inflammatory disorders.

Promotion of the transdermal delivery of protein drugs by <em>N</em>-trimethyl chitosan nanoparticles combined with polypropylene electret

“…1 However, transdermal delivery of protein drugs is severely hampered by the stratum corneum (SC), a main barrier for transdermal delivery. 2 Only a minority of lipophilic molecules could effectively penetrate SC. 3 A variety of approaches have been developed to promote the transdermal delivery of drugs.…”

Design of an Inflammation-Sensitive Polyelectrolyte-Based Topical Drug Delivery System for Arthritis

“…In addition, nanoparticulate drug delivery systems improve patient compliance by minimizing drug dosage frequency as well as providing novel and innovative treatment, facilitating targeted drug delivery and controlled release (5). There are several reports suggesting the efficiency of nanoformulation for topical drug delivery applications (6)(7)(8). Various nanoparticles were reported to be effective for the administration of anti-inflammatory drugs for the treatment of dermatitis as well as rheumatoid arthritis (9)(10)(11)(12).…”

Oleic Acid Coated Gelatin Nanoparticles Impregnated Gel for Sustained Delivery of Zaltoprofen: Formulation and Textural Characterization

“…As a vehicle they have a better potential to administer drug topically as compared to ointment because they are non-sticky require low energy during the formulation, they are stable and have an aesthetic value. 6 Polymeric nanoparticles release the drugs mostly in subcutaneous layer of skin, by surface modification of GNP with oleic acid as a penetration enhancer helps to improved drug permeation through skin. 7 To improve the drug absorption from the skin surface nanoparticulate carriers have proven to be advantageous & effective.…”