Topical Drug Delivery Systems Research Articles

Formulation and Evaluation of Niosomal Gel for Treatment of Acne

A skin disease, like acne, is very common and normally happens to everyone at least once in their lifetime. The structure of the stratum corneum is often compared with a brick wall, with corneocytes surrounded by the mortar of the intercellular lipid lamellae. Acne vulgaris is a chronic inflammatory dermatosis which is notable for open and/or closed comedones (blackheads and whiteheads), and inflammatory lesions including papules, pustules, or nodules. It is a disorder of sebaceous follicles which are special pilosebaceous units located on the face, chest, and back. Skin is one of the most readily available organs on human body for topical management and is the major route of topical drug delivery system. Topical drug administration is a localized drug delivery system everywhere in the body during ophthalmic, vaginal, rectal and skin as topical routes. SA niosomes gel delivery system (SANG1 to SANG5) as a dispersed system, which consists of small droplets and well distributed in to immiscible vehicle. Niosome salicylic acid was prepared by Reverse phase evaporation method using cholesterol and span 80 and tween 20. Niosome were evaluated for vesicle shape, size determination, Entrapment efficiency and in-vitro drug release study. The result concluded that SANG5 was best formulation with Carbopol 940 (2g), PVP, nutmeg oil base. The drug release profile and release kinetics are two important characteristics of the dosage forms, which play an important role for describing dissolution profile of dosage form.
 Keywords: Topical drug delivery, Acne vulgaris, Niosomes, Gel, Carbopol 940, nutmeg oil

Formulation and Evaluation of Ciprofloxacin, Miconazole, and Fluocinolone Acetonide Nanotechnology Based Ointment for Topical Drug Delivery System

Nanotechnology is a multidisciplinary field of science and engineering that deals with the manipulation and application of materials and structures at the nanoscale, typically involving objects with dimensions less than 100 nanometers. This emerging technology has revolutionized various industries, from electronics and medicine to materials science and energy production, by enabling scientists and engineers to work at the molecular and atomic levels.This research fully focused on the nanotechnology based drug delivery system.

The Formulation and Evaluation of Deep Eutectic Vehicles for the Topical Delivery of Azelaic Acid for Acne Treatment.

The current work was aimed at the development of a topical drug delivery system for azelaic acid (AzA) for acne treatment. The systems tested for this purpose were deep eutectic systems (DESs) prepared from choline chloride (CC), malonic acid (MA), and PEG 400. Three CC to MA and eight different MA: CC: PEG400 ratios were tested. The physical appearance of the tested formulations ranged from solid and liquid to semisolid. Only those that showed liquid formulations of suitable viscosity were considered for further investigations. A eutectic mixture made from MA: CC: PEG400 1:1:6 (MCP 116) showed the best characteristics in terms of viscosity, contact angle, spreadability, partition coefficient, and in vitro diffusion. Moreover, the MCP116 showed close rheological properties to the commercially available market lead acne treatment product (Skinorin®). In addition, the formula showed synergistic antibacterial activity between the MA moiety of the DES and the AzA. In vitro diffusion studies using polyamide membranes demonstrated superior diffusion of MCP116 over the pure drug and the commercial product. No signs of skin irritation and edema were observed when MCP116 was applied to rabbit skin. Additionally, the MCP116 was found to be, physically and chemically, highly stable at 4, 25, and 40 °C for a one-month stability study.

Anticancer Potential of Novel Nanoemulgel Formulations in Melanoma

Melanoma is classified as one of the most common cancers with an increasing incidence rate and the conventional treatment options that come with undesirable effects decrease the life quality of patients. Herein, as an alternative therapy option for systemic administration, Carbopol-based nanoemulgel formulations for local delivery were designed. Topical drug delivery systems containing Oxaliplatin, a cisplatin derivative anticancer drug used in the treatment of colorectal cancers, were evaluated for their potential for melanoma treatment. Nanoemulgel formulations with particle size under 300 nm were prepared and characterized in terms of droplet size, zeta potential and liquid crystal formation. The viscosity, as a critical attribute for topical drug delivery systems, was also evaluated, and pseudoplastic behavior of these novel drug delivery systems were confirmed. The controlled drug release pattern was shown with in vitro drug release studies with a significant difference from oxaliplatin when applied in solution. In vitro cell viability evaluation with L929 mouse fibroblast cell line confirmed the biocompatibility of prepared formulations, and the anticancer effect of novel nanoemulgel formulations were presented in B16-F10 mouse melanoma cell line. In conclusion, the anticancer potential of Oxaliplatin nanoemulgels were shown in vitro as a therapy option for melanoma, and the advantages of emulsion and gel-based drug delivery systems were combined in a nanotechnology platform for effective and patient-friendly application of an anticancer therapy for melanoma.

Transdermal Sustained Release Properties and Anti-Photoaging Efficacy of Liposome-Thermosensitive Hydrogel System.

Drug delivery systems have become a research priority in the biomedical field. The incorporation of liposomes to hydrogels further forms more robust multifunctional systems for more effective and sustained topical drug delivery. In this study, carboxymethyl-modified chitosan/hyaluronic acid (CMC/HA, CMH) thermosensitive hydrogel is developed for sustained transdermal delivery of liposomes. Hydrogels are crosslinked by hydrogen bonding, hydrophobic interaction and electrostatic interaction. The gel properties can be regulated by substitution degree (DS), and when DS = 18.20 ± 0.67% (CMH2), the gel temperature is 37.8°C, allowing rapid gelation at body temperature (315 s). Moreover, CMH2 hydrogel has suitable spreadability (17.7-57.2cm2 ), viscosity (2133.4mPas) and porous structure, which facilitated its adhesion and application on the skin and liposomes delivery. The hydrogel can retard the liposomesrelease, and the release rate of ascorbyl glucoside (AA2G)is 33.92-49.35% in 24h. Hydrogel avoids the rapid clearance of liposomes from the skin and improved the skin retention, achieving the long-term release of bioactive components. Liposome-hydrogel system more efficiently promotes the anti-photoaging effect of AA2G on skin, reducing epidermal thickness, melanin deposition and lipid oxidative damage and increasing collagen density. Therefore, liposome-hydrogel systems are proposed as multifunctional delivery systems for sustained transdermal delivery.

Recent Update on Topical Drug Delivery Systems: Emulgel

Emulgel is an emerging topical drug delivery system that, if more effort is devoted to its formulation and development with more topically active drugs, will prove to be a boon to skin care and cosmetology. Emulgels are both O/W or W/O emulsions which might be gelled with the aid of mixing with a gelling agent. Incorporating the emulgel increases its stability and makes it controlled release system. Due to the lack of excess oil bases and insoluble excipients, it exhibits better drug release compared to other topical drug delivery systems. The presence of the gel phase makes it non-greasy and promotes good affected person cooperation. Those reviews provide knowledge approximately Emulgel such as its properties, benefits, formulations and its current research advances. All elements consisting of the choice of gelling agent, oil agent, emulsifiers affecting the stability and effectiveness of Emulgel are discussed. All rationales are defined in accordance with study conducted via numerous scientists. After anin depth examine, it could be concluded that Emulgels appear to be a better and greater effective drug delivery system compared to other topical drug delivery systems. A complete analysis of the rheological and release properties will offer insight into the capacity use of the Emulgel formulation as a drug delivery System.

An overview of emulgels for topical application

In recent years, gels have been preferentially used for cosmetics and topical pharmaceutical preparations due to their favorable characteristics, such as being greaseless, readily spreadable and easily removable. However, one
 obstacle that faced it was the inability to enclose hydrophobic compounds. Therefore, a novel approach was developed to circumvent this limitation by mixing the gel with an emulsion, which led to creation of a new topical drug delivery system known as emulgel. Emulgel preserves all favorable features of gel and provides also dual release for drug, thus can be utilized effectively in controlling release and absorption of medication after topical application. Emulgel preparation requires coherent steps, this includes preparation of emulsion and gel and determining their mixing ratio. Finally, the prepared emulgels should be evaluated to ensure their suitability and efficacy for the topical application.

Design and characterization of dual‐pronged liposome‐embedded gel for enhanced dermal delivery

AbstractThe present study aims to develop a combination of Nigella sativa seed oil (NSO) and virgin coconut oil (VCO)‐loaded liposomal gel as a topical drug delivery system for vitiligo. A 3 × 3 factorial design approach was adopted to study the effect of variables on liposome characteristics and performance. A total of nine batches were formed. The cholesterol: phospholipid (wt/wt) and drug (NSO:VCO) ratios (vol/vol) were marked as two independent variables, X1 and X2. The dependent variables selected were entrapment efficiency, vesicle size, and polydispersity index. Liposomes were fabricated by thin‐film hydration technology. A carbopol gel matrix was used to embed the optimized liposome vesicles, which were then tested for pH, viscosity, ability to spread, and stability. Better stability for topical drug delivery systems was demonstrated by the incorporation of liposomes in gel prepared from cross‐linked polyacrylate. In vitro drug release, ex vivo drug permeation and drug retention were compared between liposomal and conventional preparations. Skin permeation and skin retention studies demonstrated that the prepared liposomal gel significantly extended the penetration of drugs into the skin and retained more drugs in the skin when compared to liposomal dispersion and conventional gel formulations. The stability of the developed liposomal gel was assured at 5 ± 3°C and 25 ± 2°C. From the studies described above, it is concluded that liposomal gel is the best‐suited formulation among all the preparations examined. The enhanced epidermal localization and accumulation of therapeutic moiety on the disease site could improve the effectiveness of the treatment.

CD44 targeted indirubin nanocrystal-loaded hyaluronic acid hydrogel for the treatment of psoriasis

Despite advances in transdermal drug delivery for treating psoriasis, there are still unmet medical needs, hyaluronic acid (HA)-based topical formulations as nanocarriers, which can increase drug concentration in psoriatic skin through CD44-assisted targeting. Here, HA was utilized as a matrix for nanocrystal-based hydrogel (NC-gel) to deliver indirubin topically for psoriasis treatments. Indirubin nanocrystals (NCs) were prepared through wet media milling and were then mixed with HA to create indirubin NC/HA gels. A mouse model of imiquimod (IMQ)-induced psoriasis and M5-induced keratinocyte proliferation were established. Then, the efficacy of indirubin delivery targeted at CD44, and anti-psoriatic efficacy using indirubin NC/HA gels (HA-NC-IR group) were evaluated. The HA hydrogel network embedding indirubin NCs enhanced cutaneous absorption of poorly water-soluble indirubin. The co-localization of CD44 and HA in psoriasis-like inflamed skin was highly elevated, suggesting that indirubin NC/HA gels specifically adhered to CD44, leading to an increase in indirubin accumulation in the skin. Additionally, indirubin NC/HA gels enhanced the anti-psoriatic effect of indirubin in both a mouse model and HaCaT cells stimulated with M5. The results indicate that NC/HA gels targeting overexpressed CD44 protein can improve the delivery of topical indirubin to psoriatic inflamed tissues. This suggests that a topical drug delivery system could be a viable approach for formulating multiple insoluble natural products to treat psoriasis.

Study on stability and antifungal activity against Candida albicans of gel containing clotrimazole-loaded nanoparticles

Background: Clotrimazole (CLO) is a widely used drug for the treatment of cutaneous and mucosal fungal infections caused by Candida albicans (C. albicans). To improve the topical drug absorption, nano-sized drug delivery systems have gained significant attention, particularly for poorly soluble drugs such as CLO. This research aimed to assess the drug release capability of gel containing clotrimazole-loaded nanoparticles and evaluate its antifungal activity against C. albicans. Materials and methods: CLO (China), Eudragit RS100 (Germany), Carbopol 934P (China), and other chemicals were utilized in this study. The clotrimazole-loaded nanoparticles were prepared and incorporated into the gel formulation. The in vitro drug release profile of gel was evaluated using Franz diffusion cells. Furthermore, the antifungal efficacy against C. albicans was assessed using Potato Dextrose Agar (PDA) medium. Results: The prepared gel containing CLO-loaded nanoparticles were stable during 6-week storage, demonstrated prolonged drug release after 24 hours compared to the gel containing free CLO (51.46 ± 1.10% and 71.98 ± 1.40%, respectively), exhibited better antifungal activity against C. albicans than gel containing free CLO (31 points versus 33 points). Conclusion: The CLO-loaded nanoparticles incorporated into the gel formulation showed promising potential as a topical drug delivery system, enhancing the antifungal activity and prolonging the drug release. Key words: clotrimazole, Candida albicans, antifungal, gel, nanoparticles

Simvastatin-Loaded Nanostructured Lipid Carriers as Topical Drug Delivery System for Wound Healing Purposes: Preparation, Characterization, and In Vivo Histopathological Studies.

Simvastatin, a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, is a commonly used drug to reduce total cholesterol and low-density lipoprotein (LDL) levels. Furthermore, several mechanisms showed the wound-healing potential of statins, especially simvastatin. Simvastatin is a lipophilic drug, therefore, it has low water solubility with limited skin permeability potential. In this regard, nanostructured lipid carriers (NLCs) were recruited as novel topical drug delivery systems to enhance skin adhesion and film formation, maintain skin integrity, sustain the release of simvastatin, and prolong simvastatin skin deposition to help pressure ulcers healing and regeneration. NLCs were fabricated using the solvent diffusion evaporation technique. Drug loading, in vitro drug release, and morphological assessment on the optimized formulation were considered. Furthermore, in vivo effect of simvastatin-loaded NLCs gel on pressure ulcer healing was assessed using a rat skin model. Histopathological assessments were compared with conventional simvastatin gel and drug-free NLCs gel. Simvastatin-loaded NLC with an average diameter of 100 nm was considered as the optimum formulation. According to the results entrapment efficiency of simvastatin within the NLCs was about 99.4%. Drug release studies revealed sustained drug release from NLCs in which about 87% of the drug was slowly released during 48 hours. Animal study results confirmed that simvastatin-loaded NLCs gel has better efficacy on pressure ulcers and could significantly reduce inflammation, and promote skin regeneration compared to both drug-free NLCs and conventional simvastatin gels. Simvastatin-loaded NLCs with an average particle size of 100 nm would be a promising novel topical drug delivery system with sustained drug release potential for pressure ulcer treatment.

New Insights in Topical Drug Delivery for Skin Disorders: From a Nanotechnological Perspective.

Skin, the largest organ in humans, is an efficient route for the delivery of drugs as it circumvents several disadvantages of the oral and parenteral routes. These advantages of skin have fascinated researchers in recent decades. Drug delivery via a topical route includes moving the drug from a topical product to a locally targeted region with dermal circulation throughout the body and deeper tissues. Still, due to the skin's barrier function, delivery through the skin can be difficult. Drug delivery to the skin using conventional formulations with micronized active components, for instance, lotions, gels, ointments, and creams, results in poor penetration. The use of nanoparticulate carriers is one of the promising strategies, as it provides efficient delivery of drugs through the skin and overcomes the disadvantage of traditional formulations. Nanoformulations with smaller particle sizes contribute to improved permeability of therapeutic agents, targeting, stability, and retention, making nanoformulations ideal for drug delivery through a topical route. Achieving sustained release and preserving a localized effect utilizing nanocarriers can result in the effective treatment of numerous infections or skin disorders. This article aims to evaluate and discuss the most recent developments of nanocarriers as therapeutic agent vehicles for skin conditions with patent technology and a market overview that will give future directions for research. As topical drug delivery systems have shown great preclinical results for skin problems, for future research directions, we anticipate including in-depth studies of nanocarrier behavior in various customized treatments to take into account the phenotypic variability of the disease.

Formulation Perspectives in Topical Antifungal Drug Therapy: A Review

Topical medication delivery is the process of directly treating a cutaneous ailment or the cutaneous manifestation of a general disease by applying a pharmaceutical dosage form to the skin with the goal of reducing the drug's pharmacological or other effects to the surface of skin. A wide range of pharmacological dosage forms, such as semisolids, liquid preparations, sprays, solid powders, gels, creams, and ointments, are used in topical drug delivery systems. A gel is a cross-linked polymer network swollen in a liquid medium. Its properties depend strongly on the interaction between solid state polymer and the liquid component. Gels don't have a flow that is steady. An interlacing three-dimensional network of dispersed phase particles is created by the interaction of the polymer and the liquid dispersion medium. Because topical gel formulations are less oily and readily removed from the skin, they provide an effective medication delivery mechanism. Compared to cream and ointments, gel composition offers greater application properties and stability. One of the most frequent issues with dermatological problems is fungal infection of the skin. The most effective option for treating cutaneous infections is topical treatment. The most popular antifungals in the treatment of both local and systemic fungal infections are azoles. The benefits of topical treatment for fungal infections include less risk of systemic adverse effects and medications that are targeted to the infection site. Important actions for boosting treatment effectiveness include formulation design and optimization. The most helpful aspects of a topical medication delivery system are the medication's physiochemical characteristics and formulation type. As a result, some recent developments in formulation have been researched for the delivery of antifungal medications via the target region of the skin. This review focuses on the research that has been done so far on antifungal gel and a thorough analysis of it.
 Keywords: Topical gel, Antifungal, Drug delivery, dispersion medium, fungal infection, adverse effects

Quality-by-Design-Assisted Optimization of Carvacrol Oil-Loaded Niosomal Gel for Anti-Inflammatory Efficacy by Topical Route.

Niosomes are multilamellar vesicles that effectively transfer active ingredients into the skin's layers. To improve the active substance's penetration across the skin, these carriers are frequently utilized as topical drug delivery systems. Essential oils (EOs) have garnered significant interest in the field of research and development owing to their various pharmacological activities, cost-effectiveness, and simple manufacturing techniques. However, these ingredients undergo degradation and oxidation over time, leading to a loss of functionality. Niosome formulations have been developed to deal with these challenges. The main goal of this work was to create a niosomal gel of carvacrol oil (CVC) to improve its penetration into the skin for anti-inflammatory actions and stability. By changing the ratio of drug, cholesterol and surfactant, various formulations of CVC niosomes were formulated using Box Behnken Design (BBD). A thin-film hydration technique using a rotary evaporator was employed for the development of niosomes. Following optimization, the CVC-loaded niosomes had shown: 180.23 nm, 0.265, -31.70 mV, and 90.61% of vesicle size, PDI, zeta potential, and EE%. An in vitro study on drug release discovered the rates of drug release for CVC-Ns and CVC suspension, which were found to be 70.24 ± 1.21 and 32.87 ± 1.03, respectively. The release of CVC from niosomes best fit the Higuchi model, and the Korsmeyer-Peppas model suggests that the release of the drug followed the non-Fickian diffusion. In a dermatokinetic investigation, niosome gel significantly increased CVC transport in the skin layers when compared to CVC-conventional formulation gel (CVC-CFG). Confocal laser scanning microscopy (CLSM) of rat skin exposed to the rhodamine B-loaded niosome formulation showed a deeper penetration of 25.0 µm compared to the hydroalcoholic rhodamine B solution (5.0 µm). Additionally, the CVC-N gel antioxidant activity was higher than that of free CVC. The formulation coded F4 was selected as the optimized formulation and then gelled with carbopol to improve its topical application. Niosomal gel underwent tests for pH determination, spreadability, texture analysis, and CLSM. Our findings imply that the niosomal gel formulations could represent a potential strategy for the topical delivery of CVC in the treatment of inflammatory disease.

ASSESSMENT AND OUTCOME ON PREPARATIONS, CHARACTERIZATION OF TOPICAL TARGETED NANOSPONGE BASED DRUG DELIVERY: CRITICAL REVIEW

The pharmaceutical Industry, and most of the drugs which come from synthetic chemistry possess poor water solubility and approximately 70% of drugs fall under such category. To improve solubility, drug absorption and bioavailability are a critical lookout for the formulation scientist. The current research activity for the development of dosage forms is concentrated on the development of particulate carrier systems such as microspheres and liposomes. Nanosponge is being prioritized to control the delivery of drug/APIs/phytoconstituents to particular the skin targetting. The drug delivery to skin can be prevented through the development of nanosponge. Topical nanosponge preparation can be delivered in the form of local anesthetics, anti-fungal, anti-acne, anti-wrinkle, etc. drugs. The present study highlights the developmental stages for the topical targeted nanosponge drug delivery. The review covers a different method of preparation, and evaluation of topical nanosponge drug delivery systems.

In vitro and in vivo assessment of structural integrity for HPCD complex@Liposome nanocomposites from ocular surface to the posterior segment of the eye

Investigating the structural integrity of carriers in transit from ocular surface to ocular posterior segment is essential for an efficient topical drug delivery system. In this study, dual-carrier hydroxypropyl-β-cyclodextrin complex@Liposome (HPCD@Lip) nanocomposites were developed for the efficient delivery of dexamethasone. Förster Resonance Energy Transfer with near-infrared I fluorescent dyes and in vivo imaging system were used to investigate the structural integrity of HPCD@Lip nanocomposites after crossing Human conjunctival epithelial cells (HConEpiC) monolayer and in ocular tissues. The structural integrity of inner HPCD complexes was monitored for the first time. The results suggested that 23.1 ± 6.4 % of nanocomposites and 41.2 ± 4.3 % of HPCD complexes could cross HConEpiC monolayer with an intact structure at 1 h. 15.3 ± 8.4 % of intact nanocomposites could reach at least sclera and 22.9 ± 1.2 % of intact HPCD complexes could reach choroid-retina after 60 min in vivo, which showed that the dual-carrier drug delivery system could successfully deliver intact cyclodextrin complexes to ocular posterior segment. In conclusion, in vivo assessment of structural integrity of nanocarriers is greatly significant for guiding the rational design, higher drug delivery efficiency and clinical transformation for topical drug delivery system to the posterior segment of the eye.

The Science of Selecting Excipients for Dermal Self-Emulsifying Drug Delivery Systems.

Self-emulsification is considered a formulation technique that has proven capacity to improve oral drug delivery of poorly soluble drugs by advancing both solubility and bioavailability. The capacity of these formulations to produce emulsions after moderate agitation and dilution by means of water phase addition provides a simplified method to improve delivery of lipophilic drugs, where prolonged drug dissolution in the aqueous environment of the gastro-intestinal (GI) tract is known as the rate-limiting step rendering decreased drug absorption. Additionally, spontaneous emulsification has been reported as an innovative topical drug delivery system that enables successful crossing of mucus membranes as well as skin. The ease of formulation generated by the spontaneous emulsification technique itself is intriguing due to the simplified production procedure and unlimited upscaling possibilities. However, spontaneous emulsification depends solely on selecting excipients that complement each other in order to create a vehicle aimed at optimizing drug delivery. If excipients are not compatible or unable to spontaneously transpire into emulsions once exposed to mild agitation, no self-emulsification will be achieved. Therefore, the generalized view of excipients as inert bystanders facilitating delivery of an active compound cannot be accepted when selecting excipients needed to produce self-emulsifying drug delivery systems (SEDDSs). Hence, this review describes the excipients needed to generate dermal SEDDSs as well as self-double-emulsifying drug delivery systems (SDEDDSs); how to consider combinations that complement the incorporated drug(s); and an overview of using natural excipients as thickening agents and skin penetration enhancers.

Antibacterial activity of cream, ointment, and emulgel of Ocimum basilicum L. essential oil against Propionibacterium acnes

Propionibacterium acnes is bacteria that is commonly found on healthy human skin. However, unbalanced hormonal conditions can lead to excessive growth of P. acnes, a bacteria causing acne. Previous research reported that Ocimum basilicum L. essential oil (BEO) has activity against P. acnes. Therefore, this study aims to make BEO into cream, ointment, and emulgel forms to determine its properties and antibacterial activity on those topical drug delivery systems. The preparations consisted of variations in BEO concentrations of 5%; 10%; and 15%. The three preparations were evaluated based on organoleptic, homogeneity, pH value, adhesion, and spreadability. The antibacterial activity test of the three preparations against P. acnes was carried out by the good diffusion method with the observation of the diameter of the inhibition zone (in mm). The produced cream, ointment, and cream had a typical BEO aroma, yellowish white color, and homogeneous. Based on organoleptic consistency, the texture of the thicker and longer adhesion was ointment > emulgel > cream, respectively. The pH value of the topical preparation was 5-6 and easily leveled. Antibacterial activity against P. acnes from the strongest was ointment > cream > emulgel, with a value of 14,30 + 0,30 mm; 10,54 + 0,01 mm; 3,90 + 0,04 mm, respectively.

Multilayered nanofibrous scaffold of Polyvinyl alcohol/gelatin/poly (lactic-co-glycolic acid) enriched with hemostatic/antibacterial agents for rapid acute hemostatic wound healing

Electrospun nanofibers scaffolds show promising potential in wound healing applications. This work aims to fabricate nanofibrous wound dressing as a novel approach for a topical drug delivery system. Herein, the electrospinning technique is used to design and fabricate bioabsorbable nanofibrous scaffolds of Polyvinyl alcohol/gelatin/poly (lactic-co-glycolic acid) enriched with thrombin (TMB) as hemostatic agent and vancomycin (VCM) as anti-bacterial agent for a multifunctional platform to control excessive blood loss, inhibit bacterial growth and enhance wound healing. SEM, FTIR, XRD, in vitro drug release, antimicrobial studies, biofilm, cell viability assay, and in vivo study in a rat model were used to assess nanofiber’s structural, mechanical, and biological aspects. SEM images confirms the diameter of nanofibers which falls within the range from 150 to 300 nm for all the batches. Excellent swelling index data makes it suitable to absorb wound exudates. In-vitro drug release data shows sustained release behavior of nanofiber. Nanofibers scaffolds showed biomimetic behavior and excellent biocompatibility. Moreover, scaffolds exhibited excellent antimicrobial and biofilm activity against Staphylococcus aureus. Nanofibrous scaffolds showed less bleeding time, rapid blood coagulation, and excellent wound closure in a rat model. ELISA study demonstrated the decreasing level of inflammatory markers, such as TNF-α, IL1β, and IL-6, making formulation promising for hemostatic wound healing applications. Finally, the study concludes that nanofibrous scaffolds loaded with TMB and VCM have promising potential as a dressing material for hemostatic wound healing applications.

Development and Optimization of Guggal Extract Loaded Ultradeformable Vesicles using Central Composite Design for Improving Antioxidant Potential

Background: After almost 30 years of study, it is a scientific fact that inflammation is the root cause of arthritis. Objective: Guggul has a beneficial role in arthritis because of its ability to neutralize the NF-kappa factor. A topical drug delivery system is beneficial to overcome the problems associated with oral drug delivery and offers several potential advantages. Ultra-deformable vesicles (UDVs) are a special type of liposome made up of phospholipids and surfactants, and they are highly flexible. Methods: In the present investigation, 20 formulations were suggested by Design Expert® 10 software (Central Composite Design) which were prepared using film hydration method with lecithin (70-90 mg), tween 80 (10–30 mg), Guggul extract (3 mg) and sonicated for 5–15 minutes. The formulation was optimized based on particle size (R₁) and maximum entrapment efficiency (R2). Results: The optimized formulation consists of 78.92 mg soya phosphatidyl choline (lecithin), 22.08 mg Tween 80, and 3 mg Guggul with a sonication time of 12.74 minutes that resulted in a particle size of 375.5 ±15.1 nm and entrapment efficiency of 80.3 ± 3.1%. Guggul UDVs showed more antioxidant activity compared to Guggul extract, control and standard. Similar results were obtained in the case of anti-arthritic activity, which was measured by egg albumin denaturation, bovine serum albumin denaturation, proteinase inhibitory action, and anti-lipoxygenase activity. The data of both activities were analyzed using an unpaired t-test to determine significant values (p < 0.05). Conclusion: These results demonstrate the potential of UDVs in the treatment of all arthritis diseases.