Diana Marcela Aragón

1. Melasma is one of the most prevalent forms of facial hyperpigmentation worldwide, characterized by its chronic, acquired, and recurrent nature, and mainly affecting women of reproductive age. Th...

Lipid‐based drug delivery systems (LBDDS) are a pharmaceutical strategy that improves the bioavailability of poorly water‐soluble drugs and reduces possible side effects, offering a wide variety of treatments for different pathologies, especially cancer treatment. This review aims to assess the current state of patents for LBDDS. A search was conducted in the Espacenet database from 2014 to 2024. Keywords included “Delivery system” and “Lipid”. Sixty‐six patents met the inclusion criteria, originating from China, Taiwan, the United States, Japan, and South Korea. Most of these patents focus on liposomes, with the majority aimed at improving characteristics related to efficiency, safety, and cancer treatment. LBDDS have shown significant promise in improving the bioavailability, safety, and efficacy of poorly water‐soluble drugs, particularly in cancer treatment and gene therapy. Patents over the past decade highlighted ongoing innovations in liposomes, nanoemulsions, and lipid‐polymer hybrid nanoparticles. While academic research is outpacing patent filings, the integration of both can drive further technological advancements. Despite challenges in scalability and regulatory concerns, LBDDS continues to be a promising platform for enhancing drug delivery and therapeutic outcomes. Practical application : This patent review highlights recent technological advances in lipid‐based drug delivery systems (LBDDS), offering researchers and developers a comprehensive overview of current industrial innovations. The findings support the identification of emerging excipients, nanocarrier architectures, and formulation strategies that can guide the design of next‐generation lipid systems with improved stability, bioavailability, and targeting efficiency. The compiled patent trends also help innovators recognize opportunities for translational research, anticipate regulatory and manufacturing challenges, and align academic developments with industrial needs. Furthermore, the review provides insights relevant to therapeutic areas such as cancer, gene therapy, and central nervous system disorders, facilitating the strategic selection of lipid carriers for specific applications. Overall, this work serves as a valuable resource for researchers aiming to accelerate the development, optimization, and commercialization of new lipid‐based pharmaceutical products.

Background: Solar ultraviolet (UV) radiation is a major contributor to skin damage, driving the demand for safer and more sustainable photoprotective systems. Mycosporine-like amino acids (MAAs) have emerged as promising natural UV filters due to their strong absorption and photostability; however, their application is limited by poor chemical stability in aqueous environments. Objective: The present study aimed to develop and optimize a nanoemulsion-based lip balm incorporating a MAAs-rich extract from Catenella sp., addressing stability limitations while enhancing photoprotective performance. Methods: A MAAs-rich extract was obtained and characterized by UHPLC-DAD, followed by cytotoxicity evaluation in NIH-3T3 fibroblasts and stability assessment under stress conditions. A water-in-oil (w/o) nanoemulsion was rationally developed using pseudo-ternary phase diagrams and optimized through a Box–Behnken experimental design, considering aqueous phase, surfactant mixture, and sonication time as key variables. The optimized nanoemulsion was subsequently incorporated into a lip balm matrix, which was formulated and optimized using a mixture design approach to evaluate thermal, mechanical, and sensory properties. Results: The extract exhibited a high MAAs content (9.53 mg g⁻¹ DW) and low cytotoxicity (IC₅₀ > 100 µg/mL), but pronounced hydrolytic instability, particularly under alkaline conditions, while remaining photostable. The optimized nanoemulsion achieved a droplet size below 200 nm and low polydispersity (PDI < 0.3). Importantly, incorporation of MAAs into nanoemulsion significantly enhanced the in vitro sun protection factor (SPF), increasing from 16.1 (extract) to 35.4, while maintaining broad-spectrum UV coverage (λc = 380 nm). The blank nanoemulsion also contributed to UV attenuation, indicating a synergistic effect of the colloidal system. The optimized lip balm formulation (33% beeswax, 40% nanoemulsion, 22% shea butter, 1% candelilla wax, 4% carnauba wax) demonstrated suitable melting behavior, mechanical resistance, and high sensory acceptance. Conclusions: This study demonstrates that nanoemulsion-based structuring combined with statistical formulation design provides an effective strategy to stabilize MAAs and enhance their photoprotective efficacy, supporting the development of high-performance, natural sunscreen products.

The search for sustainable and biocompatible alternatives to synthetic sunscreens has intensified due to concerns about the safety and environmental persistence of conventional UV filters. Although algae and bacteria have been extensively explored as sources of photoprotective metabolites, microscopic fungi remain comparatively neglected despite remarkable metabolic diversity and ecological adaptability. This review synthesizes research from 2014 to 2025 on fungal metabolites with photoprotective potential, including melanins, mycosporine-like amino acids (MAAs), carotenoids, quinones, xanthones, and alkaloids. These compounds absorb UV radiation and display complementary antioxidants, antimicrobial, and anti-inflammatory properties. Experimental evidence indicates that fungal metabolites can protect keratinocytes, fibroblasts, and reconstructed skin models from UV-induced oxidative stress and DNA damage, achieving sun protection factor (SPF) values comparable to commercial formulations. Advances in extraction, fermentation, and synthetic biology are enhancing production efficiency, while innovative delivery systems, such as nanoparticles, improve stability and dermal penetration. Extremophilic fungi and engineered yeasts stand out as promising biotechnological platforms for scalable biosynthesis. Despite remaining challenges in yield optimization, formulation stability, and regulatory validation, microscopic fungi represent a largely untapped resource for developing multifunctional, eco-friendly sunscreens and cosmeceuticals that integrate UV protection with broader skin health benefits.

Theobromine, a methylxanthine alkaloid found in Theobroma cacao, has gained growing attention for its pharmacological, therapeutic, and cosmetic potential. This systematic patent review analysed applications involving theobromine from 2000 to 2025 using the Espacenet database (IPC code A61K). Patents addressing pharmaceutical and cosmetic uses were included, while food, beverage, and synthetic process patents were excluded. Eligible documents were evaluated for therapeutic indications, mechanisms of action, and global distribution. Theobromine patents encompassed diverse applications including antitussive, anti-caries, lipid-modulating, osteogenic, uric acid-reducing, analgesic, and antihypertensive formulations. Cosmetic uses focused on skin lightening, anti-ageing, and slimming effects. The majority originated from the United States, Japan, China, and Europe. Synergistic formulations with complementary bioactives were frequent, highlighting multimodal innovation strategies. Overall, patent evidence supports theobromine as a promising multi-target compound with expanding biomedical and cosmeceutical relevance, reinforcing its emerging role in drug development and functional formulations.

Predictive in vitro dissolution methods are crucial for anticipating in vivo drug performance, particularly for poorly soluble drugs like carbamazepine. In vitro ‐ in vivo correlations (IVIVC) link dissolution characteristics to pharmacokinetics, facilitating bioequivalence studies and reducing reliance on clinical trials. This study aimed to develop a predictive in vitro dissolution method using USP Apparatus 4 for a modified‐release carbamazepine formulation, optimizing dissolution conditions by using principles of the IVIVC methodology. A Box–Behnken experimental design optimized dissolution parameters, including sodium lauryl sulfate concentration, flow rate, and glass bead quantity. IVIVC was assessed for a single formulation, using the Wagner‐Nelson deconvolution method and a two‐step scaling approach involving Levy plot transformation and time‐scale alignment. Gohel's reconvolution equation predicted absorbed fractions and plasma concentrations. The method's discriminatory power was evaluated using immediate‐release (IR) and modified‐release (MR) carbamazepine formulations. The refined IVIVC model achieved r ² = 0.9905, with AUC _0‐t and C _max prediction errors of −6.09% and −1.94%, respectively. The method effectively distinguished IR from MR formulations, with discriminatory analysis (f1, f2, DE, MDT) confirming its sensitivity. A predictive flow‐through cell dissolution method was successfully developed, providing a robust tool for bioequivalence studies and generic formulation development. This approach supports formulation optimization and increases the likelihood of successful in vivo bioequivalence outcomes.

Agro-industrial byproducts from Colombian Passiflora species represent an underexplored source of chemically diverse metabolites with promising cosmetic and pharmaceutical potential. This study investigated the chemical profiles and photoprotective potential of polar extracts obtained from byproducts (leaves, pericarps, and seeds) of six commercially relevant Passiflora species cultivated in Colombia (P. ligularis, P. edulis var. edulis, P. edulis var. flavicarpa, P. maliformis, P. quadrangularis and P. tarminiana × P. tripartita). Butanolic fractions from leaves and pericarps and hydroethanolic seed extracts were analyzed using ¹H NMR, GC-FID, GC-MS and UHPLC-qTOF. NMR profiling revealed aromatic signals mainly associated with flavonoids and stilbenoids in leaves and pericarps, while seeds exhibited abundant fatty acids, particularly linoleic acid. Molecular networking enabled the visualization of chemical diversity and supported the identification of 74 metabolites, including flavonoids, saponins, and stilbenoids, using Global Natural Products Social Molecular Networking (GNPS), SIRIUS (Version 6.0.5) software, and comparison with the literature. In vitro spectrophotometric photoprotective evaluation using the Mansur equation at 200 ppm showed that leaf extracts exhibited the highest sun protection factor (SPF) values, followed by seeds and pericarps, consistent with their phenolic composition. All active extracts demonstrated broad-spectrum protection, with high UVA ratios and critical wavelength values. These findings highlight the potential of Passiflora byproducts as sustainable sources of natural photoprotective agents for cosmetic applications.

Plant extracts and their bioactive components have garnered increasing scientific interest due to their diverse chemical profiles and potential impacts on human health

The growing demand for safe and effective natural ingredients in cosmetic formulations has prompted research into marine-derived compounds, particularly phlorotannins from brown algae. These compounds exhibit diverse bioactivities, including tyrosinase inhibition, which is relevant for the treatment of skin hyperpigmentation disorders. This study aimed to optimize the ultrasound-assisted extraction (UAE) of phlorotannins from the brown macroalga Dictyopteris justii and to evaluate the in vitro tyrosinase inhibitory activity of the resulting extract. A Box-Behnken design was employed to optimize the extraction parameters: ethanol concentration, solid-to-liquid ratio, temperature, and time. Total phlorotannin content (TPhC) was quantified using the DMBA colorimetric method, and the optimized extract was evaluated for tyrosinase inhibitory activity using a commercial colorimetric assay. The IC₅₀ of the extract was determined and compared with kojic acid. The optimal extraction conditions were identified as 70% ethanol, a 1:10 solid-to-liquid ratio, 25 °C, and 20 min. Under these conditions, the TPhC reached 2.874 ± 0.069 mg phloroglucinol equivalents per gram of dry extract, with a 9% extraction yield. Chromatographic analysis suggests the presence of hydroxypentafuhalol-B in the extract.The optimized extract showed significant tyrosinase inhibitory activity with an IC₅₀ of 0.51 mg/mL, compared to 46.61 µg/mL for kojic acid. This study demonstrates the successful optimization of UAE for obtaining a phlorotannin-rich extract from D. justii with reproducible extraction efficiency and potent tyrosinase inhibition. These findings support the potential application of D. justii extracts in the development of cosmetic products targeting hyperpigmentation.

Poor aqueous solubility is a major barrier in drug development, affecting dissolution, absorption, and systemic bioavailability. Nearly 40% of approved dru