1School of Pharmacy, Suresh Gyan Vihar University, Jaipur. Email: khutalerohan93@gmail.com; ORCID: 0009-0000-2960-0518
2Associate Professor, School of Pharmacy, Suresh Gyan Vihar University, Jaipur. Email: preeti.khulbe@mygyanvihar.com; ORCID: 0009-0000-3412-6961
*Corresponding Author: Rohan Atul Khutale, School of Pharmacy, Suresh Gyan Vihar University, Jaipur. Email: khutalerohan93@gmail.com
Breast cancer continues to be one of the most prevalent malignancies and a major contributor to cancer-related illness and death among women globally. Although tamoxifen is a well-established selective estrogen receptor modulator (SERM) widely used in managing hormone receptor–positive breast cancer, its oral administration is often limited by extensive hepatic first-pass metabolism, systemic toxicity, and poor site-specific drug targeting. The current research focused on the development and optimization of a tamoxifen-loaded nanostructured lipid carrier (NLC)–based topical gel designed to enhance localized drug delivery while minimizing systemic adverse effects. The NLCs were formulated using a melt-emulsification technique followed by ultrasonication, employing a solid–liquid lipid blend optimized for improved drug loading capacity and formulation stability.
The optimized formulation demonstrated a mean particle size of 178.4 ± 3.2 nm, a polydispersity index (PDI) of 0.287 ± 0.01, and a zeta potential of –26.8 ± 2.4 mV, confirming excellent colloidal stability. The entrapment efficiency (EE) and drug loading capacity were recorded at 86.9 ± 1.7% and 12.3 ± 0.9%, respectively, reflecting efficient drug encapsulation within the lipid matrix. Characterization studies using Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) revealed the absence of significant drug–lipid interactions, indicating good physicochemical compatibility.
The optimized NLC dispersion was successfully incorporated into a Carbopol-based gel, which was evaluated for pH, viscosity, spreadability, and extrudability, all of which met the required pharmaco-technical standards for topical application. In vitro release studies demonstrated a sustained drug release of up to 88.2 ± 1.5% over 24 hours, following Higuchi diffusion-controlled kinetics, indicative of diffusion-driven release behavior. Moreover, ex vivo skin permeation studies conducted using goat skin exhibited a 1.8-fold enhancement in drug penetration compared to a conventional tamoxifen gel formulation. Collectively, the findings confirm that the developed NLC-based topical gel provides prolonged drug release, improved formulation stability, and enhanced dermal permeation, establishing it as a localized, patient-friendly, and effective alternative to conventional oral tamoxifen therapy for the management of breast cancer.
Keywords: Tamoxifen, Nanostructured Lipid Carriers, Topical Gel, Breast Cancer, Controlled Release, Skin Permeation
How to cite this article: Khutale RA, Khulbe P. Formulation, Optimization and Characterization of Tamoxifen-Loaded Nanostructured Lipid Carriers (NLCs) Based Topical Gel for Localized Management of Breast Cancer. Int J Drug Deliv Technol. 2026;16(11s): 126-136; DOI: 10.25258/ijddt.16.11s.16
Source of support: Nil.
Conflict of interest: Nil