The purpose of this study was to develop a L-arginine-loaded cubosomal nanocarrier cream for topical anti-aging application. Glyceryl Monooleate and Poloxamer 407 cubosomes effectively encapsulated L-arginine, resulting in a nanosized structure (∼34.7 nm) with high entrapment efficiency (71.67 ± 0.81%). Optimal drug content (96 ± 0.08%), ideal viscosity (19,666 cps), and skin-compatible pH (6.4 ± 0.3) were obtained when incorporated into a cream base containing almond oil, Cosmacol ELI, and Sepineo P600. Formulation physiochemical compatibility was confirmed by FTIR and DSC study, sustained drug release (78.92% over 6 h) shown by in vitro release study. Reduced TNF-α expression indicated that the formulation did not elicit any pro-inflammatory response, whereas cell viability was found to be above 80%. Reduced MMP-1 and increased collagen I gene levels demonstrated anti-aging efficacy. Over a six-month period, stability studies confirmed that there was no phase separation. Overall, the cubosomal cream showed outstanding entrapment, stability, safety, and anti-aging potential, offering a promising non-invasive cosmeceutical approach for skin rejuvenation.
The therapeutic effectiveness of the most antihyperlipidemic drugs, particularly Biopharmaceutics Classification system Class II drugs like statins, is severely limited by their low aqueous solubility and resulting low and variable oral bioavailability (e.g. ∼5% for simvastatin). Deep Eutectic solvents and Therapeutic Deep Eutectic System are explored in this review as an environmentally friendly and innovative next-generation platform designed to overcome these fundamental biopharmaceutical limitations. These systems function as good solubilizers, improving the dissolution rate and the thermodynamic stability of antihyperlipidemic drugs significantly. This directly enhances the drug absorption kinetics, resulting in more predictable and enhanced oral bioavailability. Commercialization of DESs still faces major challenges. Large-scale-up is difficult because their high viscosity reduces mixing and mass transfer efficiency. Also, a complete evaluation of their cytotoxicity, biodegradability, and long-term thermal stability is still needed to ensure their safe and sustainable use as effective pharmaceutical excipients.
Over the past years, solid lipid nanoparticle delivery systems have become popular. An attractive colloidal carrier system with several applications and unique qualities, SLN seems to be. It has gained popularity due to its tolerance, increased potency, and lower levels of toxicity as well as the miracles it has achieved in treating various diseases including cancer and TB. SLN-incorporated medications are patient-compliant, easy to produce, and offer several benefits. It is cost-effective and provides administration through several routes. Solid lipid nanoparticles overcome the drawbacks of colloidal carriers and are attracting much attention from formulators. There are several methods for producing lipid nanoparticles, high and low-temperature homogenization, solvent injection, ultrasonication, and spray-drying processes have all become more popular. Because of their comprehensive positive benefits, including skin hydration, occlusion, increased bioavailability, and skin targeting, SLNs have significant potential in the pharmaceutical and cosmetics industries. This article discusses the prospective contributions of SLNs to the delivery system to attract readers' interest in SLNs. Easy production, biocompatibility, scale-up feasibility, non-irritating, increased drug loading capacity, and stability are the main characteristics of SLN that make them a viable drug delivery technology.
ABSTRACT Alzheimer's disease (AD) remains one of the most challenging neurodegenerative disorders to treat due to its multifactorial pathology and limited efficacy of current therapies. Although recent advances have focused on amyloid‐targeting strategies, effective disease modification is hindered by poor brain penetration, unfavorable pharmacokinetics, and inability to address multiple pathological pathways simultaneously. Organometallic‐based drug delivery systems have emerged as promising multifunctional platforms that combine the unique properties of metal‐containing compounds with advanced nanocarrier technologies. This review highlights recent developments in organometallic therapeutics and delivery strategies for AD, focusing on pharmaceutical design, blood‐brain barrier transport, controlled drug release, and neurotherapeutic potential. Various delivery platforms, including nanoparticles, liposomes, dendrimers, polymer conjugates, and metal‐organic frameworks, are discussed in relation to their ability to enhance drug stability, biodistribution, targeting efficiency, and therapeutic efficacy. The therapeutic relevance of these systems is further examined through their capacity to modulate amyloid‐β aggregation, oxidative stress, metal dyshomeostasis, tau pathology, and neuroinflammation. Preclinical evidence suggests that organometallic‐based platforms offer advantages over conventional approaches by integrating targeted delivery with intrinsic therapeutic activity. Despite challenges related to safety, scalability, and regulatory translation, continued advances in material design and translational research may facilitate development of clinically viable disease‐modifying therapies for AD.
OBJECTIVE:The goal of this study was to create and optimize a topical cream based on cubosomes for improved dermal delivery and stability of ferulic acid, a strong antioxidant with anti-hyperpigmentation properties that is limited by low photostability and skin permeability. SIGNIFICANCE:Improving the stability of ferulic acid and regulating its skin distribution is crucial for its successful application in cosmeceutical formulations. Cubosomal nanocarriers offer a viable way to enhance photostability, solubility, and sustained release, improving therapeutic efficacy while preserving skin safety. METHODS:Glyceryl monooleate and Poloxamer 407 were used to create ferulic acid-loaded cubosomes. The effects of almond oil and Sepineo P600 on viscosity and drug content were assessed using the Box-Behnken design to optimize cream formulation. Particle size analysis, entrapment efficiency, Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and rheological investigations were all part of the characterization. To clarify release mechanisms, kinetic models were fitted to in vitro release data. Tyrosinase inhibition studies evaluated the effectiveness of anti-hyperpigmentation, while MTT and RT-PCR assays were used to assess biocompatibility. RESULTS:The optimized formulation developed nanosized particles with thixotropic flow behavior, skin-compatible pH, and high entrapment efficiency. Diffusion-controlled delivery was indicated by release following first-order and Higuchi kinetics, although super case-II transport was suggested by Korsmeyer-Peppas analysis (n = 1.105). The cream showed moderate tyrosinase inhibition, TNF-α expression suppression, and non-cytotoxic behavior. CONCLUSION:Ferulic acid's potential as a safe and efficient cosmeceutical for skin-brightening applications is supported by the cubosomal cream's significant improvements in solubility, photostability, and prolonged dermal application.
This study aimed to improve the dissolution profile of two poorly soluble drugs, atorvastatin calcium and fenofibrate, through cocrystallization via carefully selected coformers. Five different coformers were screened via a molecular docking approach with the PyRx virtual screening tool. Binding energy and hydrogen bond formation data identified para-aminobenzoic acid (PABA) as the most suitable coformer for cocrystal formation. The cocrystallization process was carried out via the liquid-assisted grinding method. The resulting cocrystals were characterized via Fourier transform infrared (FT-IR), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), and scanning electron microscope (SEM) techniques. A detailed evaluation of fenofibrate, atorvastatin calcium, and fenofibrate−atorvastatin calcium-PABA multidrug cocrystals revealed improved solubility compared with that of the pure drugs. Characterization through FT-IR confirmed interactions between the drugs and the coformer, whereas PXRD, DSC, and SEM analyses supported the formation of a distinct crystalline phase. An in vitro dissolution study demonstrated a significant increase in the dissolution rate of the cocrystals. The findings concluded that cocrystals prepared with PABA via the liquid-assisted grinding method successfully improved the solubility of atorvastatin calcium and fenofibrate, providing a promising approach to address the challenges associated with poorly soluble drugs. The novelty lies in the strategic combination of two lipid-lowering agents into a single multicomponent crystal system, offering improved solubility, dissolution rate, and potential bioavailability compared to their standalone forms. This work pioneers the application of pharmaceutical cocrystallization for dual-drug delivery in dyslipidemia management, offering a promising platform for fixed-dose combination therapies with enhanced patient compliance and therapeutic synergy.
This review explores the field of multipulse drug delivery systems, emphasizing their potential to transform drug administration and improve therapeutic outcomes. Multipulse systems provide controlled and sustained medication release by emulating the body's natural rhythms and utilizing advanced technologies such as stimuli-responsive systems, artificial intelligence, and nanotechnology. The review examines the classification, mechanisms, and benefits of multipulse systems, highlighting their significance in chronic disease management and personalized medicine. Integrating artificial intelligence with personalized medicine enables the development of customized drug delivery systems that improve efficacy, reduce side effects, and enhance patient compliance. As we advance toward the era of precision medicine, the combination of technological and pharmaceutical innovations shows great promise for optimizing patient care and treatment outcomes.
In a recent study, the objective was to select an appropriate co-former and investigate its impact on the formation of co-crystals involving Camylofin dihydrochloride and Fumaric acid. To determine a suitable co-former, a molecular docking study was conducted, and among the compounds evaluated, fumaric acid exhibited the highest number of hydrogen bonds formed with Camylofin dihydrochloride and demonstrated a favorable Glide score of -5.21 kcal/mol. The kneading method was employed after optimizing the molar ratio of Camylofin dihydrochloride to Fumaric acid, which was found to be 1:1, 1:2, and 1:3. The resulting Camylofin dihydrochloride co-crystals underwent various analytical techniques, including Fourier Transform Infrared Spectroscopy, Scanning Electron Microscopy, Powder X-ray Diffraction, and Differential Scanning Calorimetry. The Camylofin dihydrochloride - Fumaric acid co-crystals, immediate-release tablets were formulated. Stability analysis demonstrated that the final batch F5 remained stable under accelerated ambient stability conditions (40°C±2°C, 75% RH±5%RH) and accelerated stability conditions (25°C±2°C). In conclusion, the co-crystal technology utilized in this study successfully improved the stability of Camylofin dihydrochloride without altering its chemical composition. This approach holds significant potential for enhancing the performance and characteristics of pharmaceutical formulations, thereby contributing to the development of more effective and stable medications.
IntroductionThis review examines the impact of allergic rhinitis (AR) on health, emphasizing precision medicine as a transformative approach, with AR treatments to individual factors and explores allergen immunotherapy (AIT) as a disease-modifying strategy, stressing adherence to 2019 ARIA care pathways. The role of digital technologies and mobile health tools in supporting patient-centered care is emphasized. Challenges and future prospects, including improved AIT adherence and novel biomarkers, are addressed.Area coveredThis article provides a comprehensive overview of personalized medicine, encompassing its definition, key components, and transformative impact on healthcare. It explores the role of next-generation sequencing in advancing personalized medicine, highlighting potential benefits and challenges in healthcare system implementation. Additionally, the article explores the underlying mechanisms of allergic rhinitis, the efficacy of allergen immunotherapy, and the utilization of mobile apps to improve adherence and self-care.Expert opinionIt also delves into the pathophysiology of AR and the use of innovative technologies and advancements in the AR to improve patient care. The insights presented in this article are valuable for understanding the evolving landscape of precision medicine and its impact on AR.
Aim: The study aims to evaluate the anti-angiogenic and cytotoxic properties of Carissa carandas Linn., a medicinal plant traditionally used in India for various ailments. Method: The plant's leaf extracts were prepared using methanol and n-hexane solvents and subjected to phytochemical analysis, revealing the presence of compounds like tannins, triterpenoids, and flavonoids. The antioxidant potential of the extracts was assessed, with the fruit extract showing remarkable scavenging activity against free radicals. The anti-angiogenic activity was examined using the Chorioallantoic Membrane (CAM) assay. Cytotoxicity was determined through the Brine Shrimp Lethality Assay (BSL. Results: The Chorioallantoic Membrane (CAM) assay demonstrated significant inhibition of blood vessel formation by the plant extracts. Cytotoxicity assays indicated that both methanol and n-hexane extracts contain potent bioactive constituents, albeit less potent than the standard potassium dichromate. Conclusion: The findings suggest that Carissa carandas Linn. possesses significant anti-angiogenic and cytotoxic properties, supporting its traditional use in medicine and highlighting its potential as a source of novel anticancer compounds. The study underscores the importance of scientific validation of medicinal plants' therapeutic properties and contributes to the growing interest in natural products for cancer treatment.
Millions of people around the world fall within the age group of 35 and above; having fluctuating lifestyles, increased exposure to blue light, and a faster-depleting ozone layer that enhances entry of UVA and UVB rays in the skin which tends to age faster leading into collagen degradation that results in fine lines and decreased cell senescence. The goal of skin rejuvenation is to have healthy skin. Cosmeceuticals incorporating retinoids have been increasingly used over the past few years to promote collagen synthesis and rejuvenate the skin. Photo-induced and chronological aging processes are decelerated with retinoid application that endorses skin elasticity by free radical neutralization, new cell growth, and blood vessel promotion within the skin to help fight pigmentation and reduce fine lines. Retinoids are commercially available as creams and serums for topical application. Nanotechnology is used in the development of retinoids to counteract adverse reactions like skin irritation and purging to improve its stability, efficacy, and acceptability. Emerging studies on retinoids include formulating them within liposomes, solid lipid nanoparticles, nano-emulgels, and hydrogels. This review details understanding the aging process, the mechanism of action of retinoids to counterfeit aging, and the potential use of nanotechnological delivery in cosmeceuticals.
The Cuscuta reflexa Roxb, belonging to the family Convolvulaceae is a perennial, leafless, golden-yellow parasitic herbaceous plant is one such promising herbal medicine useful in the treatment of infection, inflammation and cancer. It has been documented for anticancer, anti-inflammatory, antibacterial, antimicrobial, immunomodulatory, anti-asthmatic, antidiabetic, antidiarrheal, antiemetic, antiepileptic, antifungal, antiviral, antipyretic, antimutagenic activity, anti-steroidogenic activity, larvicidal activity. Inflammation is a biological response produced by the immune system initiated by various factors including pathogens such as bacteria, viruses or fungi infecting specific tissues. The etiological factors such as tissue injury, cell death, malignancy, ischemia and degeneration result in the inflammatory conditions. Chronic inflammation has been connected to carcinogenesis and metastatic processes, according to research. Compounds that can block or change inflammatory reactions offer a lot of promise for cancer management, prevention, and treatment. This review provides a detailed review of the literature on the pharmacological activities of Cuscuta reflexa with a special emphasis on anticancer, anti-infective, anti-inflammatory, immunomodulatory and anticancer activities of Cuscuta reflexa.
Dipyridamole (DYP) is potent drug that prevents the thromboembolic risk. It has been clinically used for chronic treatment of angina pectoris treatment and during the valve replacement. heart valve replacement and long-term angina pectoris treatment and is well absorbed in the stomach with BCS class II drug and low oral bioavailability. The present research investigation was focused on the formulation of matrix tablets of Dipyridamole cocrystals and the evaluation of In vivo anticoagulant activity. The results of the study showed that the formulated matrix tablets of dipyridamole cocrystals showed improved efficacy in comparison with the plain drug by enhancing the pre-compression parameters such as bulk density, tap density, Carr's index, angle of repose and Hausner's ratio and post-compression parameters like thickness and weight variation, hardness and friability, In vitro dissolution parameters. The improved efficacy was confirmed by improvement in the pharmacodynamic parameters such as cutaneous bleeding time and clotting time indicative of enhanced bioavailability of dipyridamole. Thus, it can be concluded that the dipyridamole matrix tablets prove to be more effective in producing the anticoagulant effect in clinical practice as compared to the plain drug resulting in more patient compliance.
Pharmaceutical research is always looking for novel ways to distribute drugs and developing these methods to increase the effectiveness of existing medications. The physicochemical characteristics of the drug determine the dose form. Lipophilic API development is a result of recent discoveries in high-throughput screening. A topical broad-spectrum antifungal agent is luliconazole. Due to its lower water solubility, topical administration is limited, and topical absorption is confined. The stratum corneum’s lipid phase’s solubility of the medication also serves as a rate-limiting step for penetration. Because fungal infections impact the skin’s epidermis, dermis, and deeper layers, medicine administration must be tailored to target high drug concentrations at the layers of the epidermis and dermis
Breast cancer has remained a serious health concern globally for women despite the healthcare advances which have enabled early diagnosis and treatment. Due to its metastatic ability and development of resistance to chemotherapies, triple-negative breast cancer is an extremely challenging subtype to treat. Targeted and optimized therapy is imperative as these tumors have higher recurrence rates than other types of breast cancers. This review is focused on the novel therapeutic strategies that have been proposed for the treatment of these aggressive cancers including alternative approaches like patient selection using biomarkers, metabolic reprogramming and development of smart drug delivery systems (SDDS) using targeted nanoparticles to treat the tumors as well as ensure prevention of recurrence. All of these approaches are aimed towards removing and treating the malignancies of triple-negative breast cancer (TNBC) and optimizing the therapies according to the patient cohorts. Further research is, however, necessary for the designing of an effective therapeutic regimen for patient sub-groups suffering from TNBC.
The current applications of nanomedicine span from the treatment of an infection right up to the treatment of cancer. Lipid nanoparticles (LNPs) have established themselves as reliable delivery systems for delivering therapeutic agents including nucleic acids since they prevent in vivo degradation of nucleic acids and facilitate their target-specific delivery. The mRNA is one such nucleic acid that is delivered by the LNPs for the treatment of infectious diseases. This review provides a detailed insight into the concept of messenger RNA (mRNA) vaccines, their mechanism of action, manufacturing process, critical considerations in the formulation, development, and manufacturing of these vaccines, and explains the vital role of LNPs in the development of these vaccines. Certain shortcomings of the lipid nanoparticle-mRNA vaccine concerning the in vitro stability of the mRNA and the LNP have also been highlighted in this review.
Dabigatran Etexilate Mesylate (DEM), a salt of prodrug dabigatran etexilate, is a potent, oral, reversible and direct thrombin inhibitor with low oral bioavailability.The present research investigation focused on the formulation of immediate release (IR) tablets of DEM cocrystals and evaluation of In vivo anticoagulant activity.The results of the study showed that the formulated IR tablets of DEM showed improved efficacy in comparison with the plain drug by enhancing the pre-compression parameters such as bulk density, tap density, Carr's index, angle of repose and Hausner's ratio and post-compression parameters like thickness and weight variation, hardness and friability, In vitro dissolution parameters.The improved efficacy was confirmed by improvement in the pharmacodynamic parameters such as cutaneous bleeding time and clotting time indicative of enhanced bioavailability of dabigatran.Thus, it can be concluded that the IR tablets of dabigatran cocrystals can be proven to be more effective in producing the anticoagulant effect in clinical practice as compared to the plain drug resulting in more patient compliance.
The current applications of nanomedicine span from the treatment of an infection right up to the treatment of cancer. Lipid nanoparticles (LNPs) have established themselves as reliable delivery systems for delivering therapeutic agents including nucleic acids since they prevent in vivo degradation of nucleic acids and facilitate their target-specific delivery. The mRNA is one such nucleic acid that is delivered by the LNPs for the treatment of infectious diseases. This review provides a detailed insight into the concept of messenger RNA (mRNA) vaccines, their mechanism of action, manufacturing process, critical considerations in the formulation, development, and manufacturing of these vaccines, and explains the vital role of LNPs in the development of these vaccines. Certain shortcomings of the lipid nanoparticle-mRNA vaccine concerning the in vitro stability of the mRNA and the LNP have also been highlighted in this review.