Nanostructured Lipid Carrier–Mediated Transdermal Delivery of Aceclofenac Hydrogel Present an Effective Therapeutic Approach for Inflammatory Diseases

Abstract

Aceclofenac (ACE), a cyclooxygenase-2 inhibitor, is the derivative of the diclofenac group that has been in use for the symptomatic treatment of systemic inflammatory autoimmune disease, rheumatoid arthritis (RA). Partial solubility, high lipophilic nature, and stability challenge its use in developing topical formulations. Hence, we developed and characterized nanostructured lipid carrier (NLC)–based ACE (ACE-NLC) hydrogel for an efficient transdermal delivery. NLC microemulsion was prepared using different lipids by various methods and was characterized with respect to particle size, zeta potential, surface morphology, and drug encapsulation efficiency. The optimized NLC formulation was incorporated into Carbopol® 940 gel, and this arrangement was characterized and compared with the existing marketed gel (Mkt-gel) formulation to assess in vitro drug release, rheology, texture profile, in vivo skin retention and permeation, and stability. Furthermore, prepared and characterized ACE-loaded NLC formulation was evaluated for skin integrity and fitted in a dermatokinetic model. The results of this study confirmed the spherical shape; smooth morphology and nanometric size attested by Zetasizer and scanning and transmission electron microcopy; and stability of the ACE-NLC formulation. The ACE-NLC-gel formulation showed good rheological and texture characteristics, and better skin distribution in the epidermis and dermis. Moreover, ACE-NLC permeated deeper in the skin layers and kept the skin integrity intact. Overall, NLC-based gel formulation of ACE might be a promising nanoscale lipid carrier for topical application when compared with the conventional Mkt-gel formulation.

Enhanced Transdermal Delivery of Pranoprofen Using a Thermo-Reversible Hydrogel Loaded with Lipid Nanocarriers for the Treatment of Local Inflammation

“…TEWL values were significantly reduced in all cases, while SCH was slightly increased. These results suggest that this formulation does not cause destabilization or damage to the skin surface and acts as an occlusive moisturizer that physically prevents transepidermal water loss and thus increases the skin hydration, possibly due to the lipid composition of the nanocarriers and the chemical nature of Pluronic ® F127 [21,36].…”

Recent advances on transdermal delivery systems for the treatment of arthritic injuries: From classical treatment to nanomedicines

“…Triptolide was loaded to the NLCs to treat RA rats and the Triptolide‐loaded NLCs showed a comparable anti‐arthritic efficacy to commercial Diclofenac sodium gel in AIA rats. More recently, Garg et al (2021) developed another NLCs to deliver Aceclofenac, also a COX‐2 inhibitor.…”

An Innovative Formulation Based on Nanostructured Lipid Carriers for Imatinib Delivery: Pre-Formulation, Cellular Uptake and Cytotoxicity Studies

“…The entrapment efficiency (EE) and loading capacity (LC) of IMT in NLCSs were determined by using a dialysis bag (Spectrum Ltd., Shanghai, China) with 8000-12,000 Da of molecular weight [9]. For that, 1 mL of NLCSs containing IMT was put into dialysis bags.…”

“…As a result, the drug molecule has a better accommodation in the NLCSs. In addition, these systems improve the drug loading capacity, reduce drug expulsion during storage, provide high drug encapsulation efficiency and cope with the drawback of drug expulsion from the lipid phase [7][8][9].…”