Delivery Of Anti-inflammatory Drugs Research Articles

ROS Responsive Cerium Oxide Biomimetic Nanoparticles Alleviates Calcium Oxalate Crystals Induced Kidney Injury via Suppressing Oxidative Stress and M1 Macrophage Polarization.

Emerging studies have demonstrated that M1 macrophage polarization and oxidative stress play important roles in calcium oxalate (CaOx) induced kidney injury, which leads to increased crystals deposition. ROS scavenging nanozymes and kidney-targeted nanoparticles for antioxidant drugs delivery have emerged as an arisen methodology for kidney injury therapy. However, cell membrane biomimetic-modified nanozymes as anti-inflammatory drug delivery systems for the treatment of kidney injury is rarely reported. Herein, the ROS responsive red blood cell-membrane-coated resatorvid-loaded cerium oxide nanoparticles (RBCM@CeO2/TAK-242) are constructed to suppress CaOx induced kidney injury and crystals deposition. In vitro, RBCM@CeO2/TAK-242 shows effective internalization by renal tubular epithelial cells, along with demonstrated antioxidative, anti-inflammatory, and macrophage reprogramming effects. Glyoxalate(Gly)-induced renal CaOx crystals mouse model is established, RBCM@CeO2/TAK-242 shows excellent injured kidney targeting and biosafety, and could effectively suppress CaOx induced kidney injury and crystals deposition. RBCM@CeO2/TAK-242 has a dual protective effect by both inhibiting oxidative stress and modulating macrophage polarization in vivo. In addition, RNA seq analysis reveals that RBCM@CeO2/TAK-242 protects against CaOx induced kidney injury via suppressing the TLR4/NF-κB pathway. This study provides an innovative strategy for RBCM@CeO2/TAK-242 as injured kidney targeting and dual protective effects for the treatment of CaOx induced kidney injury and crystals deposition.

Engineered self-regulating macrophages for targeted anti-inflammatory drug delivery

BackgroundRheumatoid arthritis (RA) is a systemic autoimmune disease characterized by increased levels of inflammation that primarily manifests in the joints. Macrophages act as key drivers for the progression of RA, contributing to the perpetuation of chronic inflammation and dysregulation of pro-inflammatory cytokines such as interleukin 1 (IL-1). The goal of this study was to develop a macrophage-based cell therapy for biologic drug delivery in an autoregulated manner.MethodsFor proof-of-concept, we developed “smart” macrophages to mitigate the effects of IL-1 by delivering its inhibitor, IL-1 receptor antagonist (IL-1Ra). Bone marrow-derived macrophages were lentivirally transduced with a synthetic gene circuit that uses an NF-κB inducible promoter upstream of either the Il1rn or firefly luciferase transgenes. Two types of joint like cells were utilized to examine therapeutic protection in vitro, miPSCs derived cartilage and isolated primary mouse synovial fibroblasts while the K/BxN mouse model of RA was utilized to examine in vivo therapeutic protection.ResultsThese engineered macrophages were able to repeatably produce therapeutic levels of IL-1Ra that could successfully mitigate inflammatory activation in co-culture with both tissue-engineered cartilage constructs and synovial fibroblasts. Following injection in vivo, macrophages homed to sites of inflammation and mitigated disease severity in the K/BxN mouse model of RA.ConclusionThese findings demonstrate the successful development of engineered macrophages that possess the ability for controlled, autoregulated production of IL-1 based on inflammatory signaling such as via the NF-κB pathway to mitigate the effects of this cytokine for applications in RA or other inflammatory diseases. This system provides proof of concept for applications in other immune cell types as self-regulating delivery systems for therapeutic applications in a range of diseases.

Mechanistic insight into heat enhanced permeation of diclofenac and piroxicam in combination with chemical penetration enhancers across skin

The topical application of heat offers considerable potential for enhancing the delivery of non-steroidal anti-inflammatory drugs across the skin barrier. A better understanding of the mechanisms underpinning the improved skin permeation and how heat can be best used to work with complementary enhancement strategies would help to realise this potential. In this study the effect of heat on the permeation of diclofenac and piroxicam across different membranes, including human skin was investigated along with use of complementary enhancement strategies including selection of formulation pH, drug salt form and inclusion of chemical penetration enhancers. Heat alone improved drug delivery across human skin for both drugs, with larger increases for piroxicam. This increase was produced by improvements in drug release, molecular diffusivity and partitioning into the stratum corneum. In combination with chemical penetration enhancers, heat synergistically increased the skin permeation of diclofenac and piroxicam up to 13 and 40-fold respectively, with the increase in permeation being ascribed primarily to improvements in drug and enhancer partitioning into the stratum corneum. An Arrhenius plot of diclofenac permeation across skin was linear indicating that the orthorhombic to hexagonal stratum corneum lipid packing transition did not have a significant effect on skin permeation in response to heat.

Using Hybrid Nanoplatforms to Combine Traditional Anti-Inflammatory Drug Delivery with RNA-Based Therapeutics for Macrophage Reprograming.

There is growing evidence on the significant role of prolonged inflammation in triggering and progressing of numerous diseases with substantial health and socioeconomic impacts, such as musculoskeletal, cardiovascular and autoimmune disorders, and cancer. Therefore, there is an urgent need to develop therapies that can overcome the main challenges of currently used approaches, such as non-target action, partial modulation of the complex inflammatory pathways, and short-term effects, to effectively manage and resolve chronic inflammatory states. This work investigates the therapeutic synergy of clinically relevant anti-inflammatory agents approaching naïve and classically activated macrophages owing to their central role in inflammation. Aiming at human therapies, a dual-loading nanoplatform reunites molecules with different physico-chemical properties in a single system, seeking to more effectively and comprehensively regulate macrophage functions for precision cell guidance and greater versatility in disease managing. To build this platform, palmitic acid grafted chitosan, superparamagnetic iron oxide nanoparticles, the clinically approved NSAID celecoxib (also known as Celebrex®), and RNA technologies were combined into superparamagnetic polymeric micelles (SPMs). Our findings demonstrated that traditional anti-inflammatory drugs such as celecoxib and microRNA molecules were efficiently delivered by the SPMs, altering the inflammatory profile of naïve (M0φ) and M1-primed macrophages (M1φ) assessed by gene and protein expression. The impact of the dual-loaded SPMs in naïve Mφ is an interesting finding towards the modulation of the initial immune response, reducing the potential for chronic inflammation and promoting tissue healing. Collectively, these encouraging results demonstrate the promise of multi-nanomedicine strategies to enhance the efficacy of therapeutic interventions by offering a fresh approach to more precisely and carefully regulated nanotherapeutics delivery.

Systemic low-dose anti-fibrotic treatment attenuates ovarian aging in the mouse.

The female reproductive system is one of the first to age in humans, resulting in infertility and endocrine disruptions. The aging ovary assumes a fibro-inflammatory milieu which negatively impacts gamete quantity and quality as well as ovulation. Here, we tested whether the systemic delivery of anti-inflammatory (Etanercept) or anti-fibrotic (Pirfenidone) drugs attenuates ovarian aging in mice. We first evaluated the ability of these drugs to decrease the expression of fibro-inflammatory genes in primary ovarian stromal cellstreated with a pro-fibrotic or a pro-inflammatory stimulus. Whereas Etanercept did not block Tnf expression in ovarian stromal cells, Pirfenidone significantly reduced Col1a1 expression. We then tested Pirfenidone in vivo where the drug was delivered systemically via mini-osmotic pumps for 6weeks. Pirfenidone mitigated the age-dependent increase in ovarian fibrosis without impacting overall health parameters. Ovarian function was improved in Pirfenidone-treated mice as evidenced by increased follicle and corpora lutea number, AMH levels, and improved estrous cyclicity. Transcriptomic analysis revealed that Pirfenidone treatment resulted in an upregulation of reproductive function-related genes at 8.5months and a downregulation of inflammatory genes at 12months of age. These findings demonstrate that reducing the fibroinflammatory ovarian microenvironment improves ovarian function, thereby supporting modulating the ovarian environment as a therapeutic avenue to extend reproductive longevity.

Eco-friendly nanotechnology in rheumatoid arthritis: ANFIS-XGBoost enhanced layered nanomaterials

Rheumatoid arthritis (RA) is a chronic autoimmune disorder characterized by inflammation and pain in the joints, which can lead to joint damage and disability over time. Nanotechnology in RA treatment involves using nano-scale materials to improve drug delivery efficiency, specifically targeting inflamed tissues and minimizing side effects. The study aims to develop and optimize a new class of eco-friendly and highly effective layered nanomaterials for targeted drug delivery in the treatment of RA. The study's primary objective is to develop and optimize a new class of layered nanomaterials that are both eco-friendly and highly effective in the targeted delivery of medications for treating RA. Also, by employing a combination of Adaptive Neuron-Fuzzy Inference System (ANFIS) and Extreme Gradient Boosting (XGBoost) machine learning models, the study aims to precisely control nanomaterials synthesis, structural characteristics, and release mechanisms, ensuring delivery of anti-inflammatory drugs directly to the affected joints with minimal side effects. The in vitro evaluations demonstrated a sustained and controlled drug release, with an Encapsulation Efficiency (EE) of 85% and a Loading Capacity (LC) of 10%. In vivo studies in a murine arthritis model showed a 60% reduction in inflammation markers and a 50% improvement in mobility, with no significant toxicity observed in major organs. The machine learning models exhibited high predictive accuracy with a Root Mean Square Error (RMSE) of 0.667, a correlation coefficient (r) of 0.867, and an R2 value of 0.934. The nanomaterials also demonstrated a specificity rate of 87.443%, effectively targeting inflamed tissues with minimal off-target effects. These findings highlight the potential of this novel approach to significantly enhance RA treatment by improving drug delivery precision and minimizing systemic side effects.

In situ Gels for Periodontitis: An Overview

ABSTRACT A successful approach for periodontitis treatment is in situ gel administration, which delivers medication to the site of infection in a controlled and continuous manner. Researchers used components such as zein, borneol, piperine, and curcumin to create a formulation. The formulations demonstrated antimicrobial effects and were designed to target the inflammatory condition associated with dysbiosis in periodontitis. Polymers such as gellan gum, alginic acid, xyloglucan, pectin, chitosan, poly (D Lactic acid), poly (DL-lactide co glycolide), and polycaprolactone are commonly used polymers to prepare the In situ gel formulation , which enables prolonged medication and Controlled release. In the presence of ions, alginic acid gels are biocompatible. Whereas pectin gels are used in the presence of calcium ions, xyloglucan gels are used in response to temperature fluctuations. To increase the efficacy of the treatment, the studies sought to enhance gel characteristics such as gelation temperature, thickness, and drug release rate. The improved formulations showed anti-inflammatory solid effects and efficient drug delivery for periodontal conditions by significantly reducing pocket depth, plaque, and gum inflammation. The direct application of in situ gels offers targeted delivery, few side effects, and self-administration; the review focuses on the benefits, advantages, and disadvantages of in situ gel administration for periodontitis, as well as the characteristics of tooth physiology, preparation techniques, and polymers and biomarkers used. Assessments of in situ gels: To significantly improve periodontitis treatment, future research should focus on clinical studies to contribute substantially to periodontitis treatment.

Systemic low-dose anti-fibrotic treatment attenuates ovarian aging in the mouse.

The female reproductive system is one of the first to age in humans, resulting in infertility and endocrine disruptions. The aging ovary assumes a fibro-inflammatory milieu which negatively impacts gamete quantity and quality as well as ovulation. Here we tested whether the systemic delivery of anti-inflammatory (Etanercept) or anti-fibrotic (Pirfenidone) drugs attenuates ovarian aging in mice. We first evaluated the ability of these drugs to decrease the expression of fibro-inflammatory genes in primary ovarian stromal cells. Whereas Etanercept did not block Tnf expression in ovarian stromal cells, Pirfenidone significantly reduced Col1a1 expression. We then tested Pirfenidone in vivo where the drug was delivered systemically via mini-osmotic pumps for 6-weeks. Pirfenidone mitigated the age-dependent increase in ovarian fibrosis without impacting overall health parameters. Ovarian function was improved in Pirfenidone-treated mice as evidenced by increased follicle and corpora lutea number, AMH levels, and improved estrous cyclicity. Transcriptomic analysis revealed that Pirfenidone treatment resulted in an upregulation of reproductive function-related genes at 8.5 months and a downregulation of inflammatory genes at 12 months of age. These findings demonstrate that reducing the fibroinflammatory ovarian microenvironment improves ovarian function, thereby supporting modulating the ovarian environment as a therapeutic avenue to extend reproductive longevity.

Fabrication and characterization of thin self-rolling film for anti-inflammatory drug delivery

Thin films have been identified as an alternative approach for targeting sensitive site as drug delivery tool. In this work, the preparation of self-rolling thin films to form tubes for wound healing and easy placement (e.g. in the colon via colonoscopy) have been studied. We explored the use of thin films as a protective dressing combined to local release of an anti-inflammatory in order to improve drug efficacy and limit the side effects of the oral route. Non-cytotoxic poly(ethylene) glycol and poly(lactic acid) photo-crosslinkable star copolymers were used for rapid UV crosslinking of bilayered films loaded with prednisolone. The films, crosslinked under UV lamp without the need of photoinitiator, are optimized and compared in terms of water uptake, swelling ratio, final tube diameter and morphology, anti-inflammatory drug loading and release. Our studies showed the spontaneous rolling of bilayer constructs directly after immersion in water. Tubular geometry allows application of the patch through minimally invasive procedures such as colonoscopy. Moreover, the rolled-up bilayers highlighted efficient release of encapsulated drug following Fickian diffusion mechanism. We also confirmed the anti-inflammatory activity of the released anti-inflammatory drug that inhibits the pro-inflammatory cytokine IL-1β in RAW 264.7 macrophages stimulated by Escherichia coli (E. coli).

Engineered Self-Regulating Macrophages for Targeted Anti-inflammatory Drug Delivery.

Rheumatoid arthritis (RA) is a systemic autoimmune disease characterized by increased levels of inflammation that primarily manifests in the joints. Macrophages act as key drivers for the progression of RA, contributing to the perpetuation of chronic inflammation and dysregulation of pro-inflammatory cytokines such as interleukin 1 (IL-1). The goal of this study was to develop a macrophage-based cell therapy for biologic drug delivery in an autoregulated manner. For proof-of-concept, we developed "smart" macrophages to mitigate the effects of IL-1 by delivering its inhibitor, IL-1 receptor antagonist (IL-1Ra). Bone marrow-derived macrophages were lentivirally transduced with a synthetic gene circuit that uses an NF-κB inducible promoter upstream of either the Il1rn or firefly luciferase transgenes. Two types of joint like cells were utilized to examine therapeutic protection in vitro, miPSCs derived cartilage and isolated primary mouse synovial fibroblasts while the K/BxN mouse model of RA was utilized to examine in vivo therapeutic protection. These engineered macrophages were able to repeatably produce therapeutic levels of IL-1Ra that could successfully mitigate inflammatory activation in co-culture with both tissue engineered cartilage constructs and synovial fibroblasts. Following injection in vivo, macrophages homed to sites of inflammation and mitigated disease severity in the K/BxN mouse model of RA. These findings demonstrate the successful development of engineered macrophages that possess the ability for controlled, autoregulated production of IL-1 based on inflammatory signaling such as the NF-κB pathway to mitigate the effects of this cytokine for applications in RA or other inflammatory diseases. This system provides proof of concept for applications in other immune cell types as self-regulating delivery systems for therapeutic applications in a range of diseases.

Strategies to Improve the Transdermal Delivery of Poorly Water-Soluble Non-Steroidal Anti-Inflammatory Drugs.

The transdermal delivery of non-steroidal anti-inflammatory drugs (NSAIDs) has the potential to overcome some of the major disadvantages relating to oral NSAID usage, such as gastrointestinal adverse events and compliance. However, the poor solubility of many of the newer NSAIDs creates challenges in incorporating the drugs into formulations suitable for application to skin and may limit transdermal permeation, particularly if the goal is therapeutic systemic drug concentrations. This review is an overview of the various strategies used to increase the solubility of poorly soluble NSAIDs and enhance their permeation through skin, such as the modification of the vehicle, the modification of or bypassing the barrier function of the skin, and using advanced nano-sized formulations. Furthermore, the simple yet highly versatile microemulsion system has been found to be a cost-effective and highly successful technology to deliver poorly water-soluble NSAIDs.

Drug Integrating Amphiphilic Nano-Assemblies: 2. Spatiotemporal Distribution within Inflammation Sites.

The need for chronic systemic immunosuppression, which is associated with unavoidable side-effects, greatly limits the applicability of allogeneic cell transplantation for regenerative medicine applications including pancreatic islet cell transplantation to restore insulin production in type 1 diabetes (T1D). Cell transplantation in confined sites enables the localized delivery of anti-inflammatory and immunomodulatory drugs to prevent graft loss by innate and adaptive immunity, providing an opportunity to achieve local effects while minimizing unwanted systemic side effects. Nanoparticles can provide the means to achieve the needed localized and sustained drug delivery either by graft targeting or co-implantation. Here, we evaluated the potential of our versatile platform of drug-integrating amphiphilic nanomaterial assemblies (DIANAs) for targeted drug delivery to an inflamed site model relevant for islet transplantation. We tested either passive targeting of intravenous administered spherical nanomicelles (nMIC; 20-25 nm diameter) or co-implantation of elongated nanofibrils (nFIB; 5 nm diameter and >1 μm length). To assess the ability of nMIC and nFIB to target an inflamed graft site, we used a lipophilic fluorescent cargo (DiD and DiR) and evaluated the in vivo biodistribution and cellular uptake in the graft site and other organs, including draining and non-draining lymph nodes, after systemic administration (nMIC) and/or graft co-transplantation (nFIB) in mice. Localized inflammation was generated either by using an LPS injection or by using biomaterial-coated islet-like bead implantation in the subcutaneous site. A cell transplant inflammation model was used as well to test nMIC- and nFIB-targeted biodistribution. We found that nMIC can reach the inflamed site after systemic administration, while nFIB remains localized for several days after co-implantation. We confirmed that DIANAs are taken up by different immune cell populations responsible for graft inflammation. Therefore, DIANA is a useful approach for targeted and/or localized delivery of immunomodulatory drugs to decrease innate and adaptive immune responses that cause graft loss after transplantation of therapeutic cells.

Green Revolution in Pharmaceutical Formulations: Banana Peel-Derived Fast-Dissolving Tablets for Enhanced NSAID Delivery

The pharmaceutical industry is undergoing a transformative shift towards sustainable practices, and this review explores the potential of utilizing banana peel-derived materials in the development of Fast-Dissolving Tablets (FDTs) for Non-Steroidal Anti-Inflammatory Drug (NSAID) delivery. Banana peels, often discarded as waste, contain bioactive compounds with promising pharmaceutical applications. This review provides a comprehensive summary of key findings, emphasizing the biocompatibility, sustainability, and cost-effectiveness of banana peel-derived materials in pharmaceutical formulations. Taste-masking techniques and flavor enhancements are discussed as crucial considerations to enhance patient acceptability. The implications for the pharmaceutical industry extend beyond therapeutic benefits, aligning with the growing demand for environmentally conscious practices. The future outlook highlights the need for further research and development, optimization of formulations, and comprehensive evaluations to establish the safety, efficacy, and regulatory compliance of banana peel-derived FDTs. Successfully integrating these materials may set a precedent for eco-friendly drug development, fostering a green paradigm in the pharmaceutical industry.

Preparation and Investigation of a Nanosized Piroxicam Containing Orodispersible Lyophilizate.

Non-steroidal anti-inflammatory piroxicam (PRX) is a poorly water-soluble drug that provides relief in different arthritides. Reducing the particle size of PRX increases its bioavailability. For pediatric, geriatric, and dysphagic patients, oral dispersible systems ease administration. Moreover, fast disintegration followed by drug release and absorption through the oral mucosa can induce rapid systemic effects. We aimed to produce an orodispersible lyophilizate (OL) consisting of nanosized PRX. PRX was solved in ethyl acetate and then sonicated into a poloxamer-188 solution to perform spray-ultrasound-assisted solvent diffusion-based nanoprecipitation. The solid form was formulated via freeze drying in blister sockets. Mannitol and sodium alginate were applied as excipients. Dynamic light scattering (DLS) and nanoparticle tracking analysis (NTA) were used to determine the particle size. The morphology was characterized by scanning electron microscopy (SEM). To establish the crystallinity, X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) were used. A disintegration and in vitro dissolution test were performed. DLS and NTA presented a nanosized PRX diameter. The SEM pictures showed a porous structure. PRX became amorphous according to the XRPD and DSC curves. The disintegration time was less than 1 min and the dissolution profile improved. The final product was an innovative anti-inflammatory drug delivery system.

The contemplation of amylosefor the delivery of ulcerogenic nonsteroidal anti-inflammatory drugs.

This manuscript proposes an innovative approach to mitigate the gastrointestinal adversities linked withnonsteroidal anti-inflammatory drugs (NSAIDs) by exploiting amylose as a novel drug delivery carrier. The intrinsic attributes of V-amylose, such as its structural uniqueness, biocompatibility andbiodegradability, as well asits capacity to form inclusion complexes with diverse drug molecules, are meticulously explored. Through a comprehensive physicochemical analysis of V-amylose and ulcerogenic NSAIDs, the plausibility of amylose as a protective carrier for ulcerogenic NSAIDs to gastrointestinal regions is elucidated. This review further discusses the potential therapeutic advantages of amylose-based drug delivery systems in the management of gastric ulcers. By providing controlled release kinetics and enhanced bioavailability, these systems offer promising prospects for the development of more effective ulcer therapies.

Gentiopicrin-Loaded Chitosan Nanoparticles as a Topical Agent for the Treatment of Psoriasis.

Psoriasis, a chronic inflammatory skin disease induced by various factors, including genetic factors, immune factors, environmental factors, and psychological factors, is characterized by thickening of the epidermis, excessive proliferation of keratinocytes, abnormal differentiation, and an excessive inflammatory response. Traditional treatments for psoriasis still face challenges because of limited curative effects, notable side effects, and a tendency for recurrence. In contrast, topical therapy provides a favorable option for psoriasis treatment because of its noninvasive and self-administered method. In this study, gentiopicrin (Gen) is encapsulated in the liposomes to form a nanodrug, and then chitosan is covered on the nanodrug to assemble the nanodrug delivery system (CS@Gen), which is used as a topical agent for treating psoriasis. Then M5 (a mixture of five pro-inflammatory cytokines, i.e., IL-17A, IL-22, IL-1α, oncostatin M, and TNF-α)-induced HacaT cells and imiquimod-induced psoriasis mouse models are established, whose results show that CS@Gen induces apoptosis and inhibits the proliferation and cell migration of psoriasis keratinocytes. Additionally, the application of CS@Gen cream can significantly reduce epidermal thickness, diminish skin scaling, and improve other related mechanisms in mice affected by psoriasis. Meanwhile, the prepared CS@Gen can significantly reduce the expression levels of IL-17a, Cxcl2, S100a, Mki67, and other related inflammatory factors, resulting in indirectly inhibiting the inflammation of keratinocytes. In summary, the present study provides an ideal loading for an anti-inflammatory and immunomodulatory drug delivery system for the treatment of psoriasis.

MUKOADEZİF POLİMERLERİN KOLON HEDEFLİ İLAÇ TAŞIYICI SİSTEMLERDE KULLANIMI: DETAYLI BİR İNCELEME

Objective: Mucoadhesive polymers have emerged as crucial components in the realm of drug delivery systems, particularly in the context of targeted treatments within the colon. These polymers possess adhesive properties that enable them to form temporary bonds with mucosal surfaces, extending the contact time of drugs with the colonic mucosa. This review provides a comprehensive overview of mucoadhesive polymers for colon drug delivery systems. Natural polymers such as chitosan and alginate, along with synthetic counterparts like polyacrylic acid derivatives, find application in these systems. The advantages of mucoadhesive polymers lie in their ability to facilitate site-specific drug delivery, thereby minimizing systemic side effects, and in enabling controlled and sustained release of drugs for improved bioavailability. Despite these benefits, challenges including variability in mucosal conditions and the imperative need for biocompatibility must be addressed. The applications of mucoadhesive polymers span diverse medical conditions, including targeted delivery of anti-inflammatory drugs for inflammatory bowel diseases, localized administration of chemotherapeutic agents for colon cancer treatment, and precise delivery of antibiotics for colonic infections. Result and Discussion: As a promising avenue for optimizing colon drug delivery, mucoadhesive polymers offer great potential for the development of effective and well-tolerated treatments for various colonic disorders.

Organogels: "GelVolution" in Topical Drug Delivery - Present and Beyond.

Topical drug delivery holds immense significance in dermatological treatments due to its non-invasive nature and direct application to the target site. Organogels, a promising class of topical drug delivery systems, have acquired substantial attention for enhancing drug delivery efficiency. This review article aims to explore the advantages of organogels, including enhanced drug solubility, controlled release, improved skin penetration, non-greasy formulations, and ease of application. The mechanism of organogel permeation into the skin is discussed, along with formulation strategies, which encompass the selection of gelling agents, cogelling agents, and additives while considering the influence of temperature and pH on gel formation. Various types of organogelators and organogels and their properties, such as viscoelasticity, non-birefringence, thermal stability, and optical clarity, are presented. Moreover, the biomedical applications of organogels in targeting skin cancer, anti-inflammatory drug delivery, and antifungal drug delivery are discussed. Characterization parameters, biocompatibility, safety considerations, and future directions in optimizing skin permeation, ensuring long-term stability, addressing regulatory challenges, and exploring potential combination therapies are thoroughly examined. Overall, this review highlights the immense potential of organogels in redefining topical drug delivery and their significant impact on the field of dermatological treatments, thus paving the way for exciting prospects in the domain.

Emulgel: A Cutting Edge Approach for Topical Drug Delivery System.

Emulgel is considered an advanced leading form of topical drug delivery system. It possesses the quality of a dual control drug mechanism for drug release as it holds the properties of both gel as well as emulsion. Emulgel is capable of overcoming the problems of the conventional route of topical drug delivery, like low spreadability and stickiness with the delivery of hydrophobic drugs, enhanced bioavailability at the local site of action, no greasy texture, and ensuring patient compliance. An emulsion is used either w/o or o/w, and the drug can be incorporated into the suitable phase of the emulsion. After that, the emulsion is incorporated into the gel phase. Several factors like oil phase, gelling agent, and emulsifier can affect the efficacy and stability. This advancement is beneficial not only for dermatology but also for cosmetology as well. Currently, emulgel-based formulations are used for the delivery of anti-inflammatory, analgesic, anti-acne, and antifungal drugs with a wide array of exploration.

PEG-Lipid-PLGA Hybrid Particles for Targeted Delivery of Anti-Inflammatory Drugs.

Hybrid nanoparticles (HNPs) were designed by combining a PLGA core with a lipid shell that incorporated PEG-Lipid conjugates with various functionalities (-RGD, -cRGD, -NH2, and -COOH) to create targeted drug delivery systems. Loaded with a neutral lipid orange dye, the HNPs were extensively characterized using various techniques and investigated for their uptake in human monocyte-derived macrophages (MDMs) using FC and CLSM. Moreover, the best-performing HNPs (i.e., HNP-COOH and HNP-RGD as well as HNP-RGD/COOH mixed) were loaded with the anti-inflammatory drug BRP-201 and prepared in two size ranges (dH ~140 nm and dH ~250 nm). The HNPs were examined further for their stability, degradation, MDM uptake, and drug delivery efficiency by studying the inhibition of 5-lipoxygenase (5-LOX) product formation, whereby HNP-COOH and HNP-RGD both exhibited superior uptake, and the HNP-COOH/RGD (2:1) displayed the highest inhibition.