Development and Evaluation of pH-Responsive Pluronic F 127 Co-Poly- (Acrylic Acid) Biodegradable Nanogels for Topical Delivery of Terbinafine HCL

Abstract

Research aimed to develop and evaluate biodegradable, pH-responsive chemically cross-linked Pluronic F127 co-poly- (acrylic acid) nanogels for dermal delivery of Terbinafine HCL (TBH) to increase its permeability and as a new approach to treat skin fungal infections. TBH-loaded nanogels were successfully synthesized from acrylic acid (AA) and Pluronic F127 by free-radical copolymerization technique using N,N′-methylene bisacrylamide (MBA) as crosslinker and ammonium persulphate (APS) as initiator. Prepared nanogels exhibited 93.51% drug entrapment efficiency (DEE), 45 nm particle size, pH-dependent swelling and release behavior. Nanogels were characterized using different physicochemical techniques. The ex-vivo skin retention studies through rat skin showed about 42.34% drug retention from nanogels while 1% Lamisil cream (marketed product) showed about 26.56% drug retention. Moreover, skin irritation studies showed that nanogels were not irritating. Nanogels showed improved in-vitro antifungal activity against Candida albicans compared to commercial product. In-vivo studies on rats infected with Candida albicans confirmed superiority of nanogels over 1% Lamisil for eradication of fungal infection. This confirms that TBH loaded in Pluronic F127 co-poly-(acrylic acid) nanogels provided greater targetibility and cure rates of poorly soluble TBH in animal model and hence nanogels could be a potential carrier for effective topical delivery of TBH for skin fungal infection treatment.

Crosslinked PVA-g-poly(AMPS) Nanogels for Enhanced Solubility and Dissolution of Ticagrelor: Synthesis, Characterization, and Toxicity Evaluation

“…An increase in swelling was observed by increasing the monomer (AMPS) concentration (Figure e). This is due to the hydrophilic nature and ionization of AMPS over a wide pH range, which further enhanced its hydrophilicity. , By increasing the feed composition of the crosslinker (MBA), the swelling was decreased (Figure f) due to excessive crosslinking, which resulted in intertwingled polymer chains, leading to a dense and firm network, which imparted some degree of hydrophobicity that protected the nanogel from immense water penetration. , …”

“… 23 , 43 By increasing the feed composition of the crosslinker (MBA), the swelling was decreased ( Figure 8 f) due to excessive crosslinking, which resulted in intertwingled polymer chains, leading to a dense and firm network, which imparted some degree of hydrophobicity that protected the nanogel from immense water penetration. 40 , 44 …”

The Exploitation of pH-Responsive Eudragit-Coated Mesoporous Silica Nanostructures in the Repurposing of Terbinafine Hydrochloride for Targeted Colon Cancer Inhibition: Design Optimization, In Vitro Characterization, and Cytotoxicity Assessment

“…The signal at 2983 cm −1 was ascribed to the aliphatic C-H group stretching; whereas, the peak at 3043 cm −1 suggested aromatic C-H groups. In addition, TER has a characteristic peak at about 3400 cm −1 for OH and NH groups [ 49 ]. In Figure 4 b, Eud S-100 showed the sharp characteristic peak at 1750 cm −1 , indicating the stretching vibration of the C=O of the ester groups.…”