Topical Gel Formulation Research Articles

Incorporating strawberry leaf extract from waste biomass in prototype topical gel and cream formulations

Incorporating strawberry leaf extract from waste biomass in prototype topical gel and cream formulations

Cyclodextrin-Nanosponge-Loaded Cyclo-Oxygenase-2 Inhibitor-Based Topical Gel for Treatment of Psoriatic Arthritis: Formulation Design, Development, and In vitro Evaluations

Background: Psoriatic arthritis (PsA), a chronic inflammatory disease, mainly affects the joints, with approximately 30% of psoriasis patients eventually developing PsA. Characterized by both innate and adaptive immune responses, PsA poses significant challenges for effective treatment. Recent advances in drug delivery systems have sparked interest in developing novel formulations to improve therapeutic outcomes. The current research focuses on the development and evaluation of a nanosponge-loaded, cyclo-oxygenase-2 (COX-2) inhibitor-based topical gel for the treatment of PsA. Methods: Nanosponges (NSs) were prepared by using beta-cyclodextrin as a polymer and dimethyl carbonate (DMC) as a crosslinker by melting, and gels were prepared by employing carbopol and badam gum as polymers. Results: Solubility studies confirmed that the prepared nanosponges were highly soluble. FT-IR studies confirmed the formation of hydrogen bonds between lumiracoxib and beta-cyclodextrin. SEM confirmed that the prepared formulations were roughly spherical and porous in nature. The average particle size was 190.5 ± 0.02 nm, with a zeta potential of −18.9 mv. XRD studies showed that the crystallinity of lumiracoxib decreased after encapsulation, which helped to increase its solubility. The optimized nanosponges (NS2) were incorporated in an optimized gel (FG10) to formulate a nanosponge-loaded topical gel. The optimized gel formulation exhibited a homogeneous consistency, with a pH of 6.8 and a viscosity of 1.15 PaS, indicating its suitability for topical application and stability. The in vitro diffusion studies for the topical gel showed drug release of 82.32% in 24 h. The optimized formulation demonstrated significant antipsoriatic activity, as confirmed through cytotoxicity studies conducted on HaCaT cells. Conclusions: On the basis of the findings, it can be concluded that the prepared nanosponge-loaded topical gel formulation presents a promising solution for the effective management of PsA, offering enhanced drug solubility, sustained release, and improved therapeutic potential.

Engineering a Mesoporous Silicon Nanoparticle Cage to Enhance Performance of a Phosphotriesterase Enzyme for Degradation of VX Nerve Agent.

The organophosphate (OP)-hydrolyzing enzyme phosphotriesterase (PTE, variant L7ep-3a) immobilized within a partially oxidized mesoporous silicon nanoparticle cage is synthesized and the catalytic performance of the enzyme@nanoparticle construct for hydrolysis of a simulant, dimethyl p-nitrophenyl phosphate (DMNP), and the live nerve agent VX is benchmarked against the free enzyme. In a neutral aqueous buffer, the optimized construct shows a ≈2-fold increase in the rate of DMNP turnover relative to the free enzyme. Enzyme@nanoparticles with more hydrophobic surface chemistry in the interior of the pores show lower catalytic activity, suggesting the importance of hydration of the pore interior on performance. The enzyme@nanoparticle construct is readily separated from the neutralized agent; the nanoparticle is found to retain DMNP hydrolysis activity through seven decontamination/recovery cycles. The nanoparticle cage stabilizes the enzyme against thermal denaturing and enzymatic (trypsin) degradation conditions relative to free enzyme. When incorporated into a topical gel formulation, the PTE-loaded nanoparticles show high activity toward the nerve agent VX in an ex vivo rabbit skin model. In vitro acetylcholinesterase (AChE) assays in human blood show that the enzyme@nanoparticle construct decontaminates VX, preserving the biological function of AChE when exposed to an otherwise incapacitating dose.

Development and Optimization of Transferosomal Gel for Efficient Topical Delivery of Berberine Hydrochloride

Background: Berberine is an isoquinoline alkaloid with potent anti-inflammatory effects. However, its therapeutic efficacy is often restricted by its poor solubility, absorption, and permeability, especially in topical applications. Transferosomes are elastic vesicular carriers with high skin permeability values and retention, making them suitable for encapsulating hydrophilic and lipophilic actives. Objective: The objective of this research was to develop a transferosome-based topical gel formulation of Berberine hydrochloride (BER) to improve its skin permeability and anti-inflammatory efficacy. Method: The thin film hydration method was used to formulate the BER transferosomes. The effects of independent variables, amount of BER in lipid phase (X1), and lipid (Phospholipon 90G) to surfactant ratio (X2) on BER entrapment and vesicle size were studied using face-centered central composite design. The characterization was performed using differential scanning calorimetry, transmission electron microscopy, and X-ray diffraction. The optimized batch (F5) was incorporated in Carbopol gel and further investigated for viscosity, in vitro and ex-vivo diffusion, skin retention by tape stripping, and in-vivo anti-inflammatory efficiency. Results: The formulation optimized with 50 mg of drug and a 5:1 lipid-to-surfactant ratio (F5) demonstrated higher drug entrapment efficiency (72.11%) and lower vesicle size (77.9 nm). TEM validated the spherical vesicle morphology, whereas DSC and XRD analysis confirmed the molecular entrapment of BER within the phospholipid vesicles. The transferosomal gel demonstrated improved BER diffusion (0.63 mg/cm2) confirmed by in vitro and ex-vivo diffusion experiments that revealed a 6-fold increase in flux and permeability coefficient (0.1053 mg. cm-2.h-1). The drug release from transferosome gel was non-Fickian in nature (n = 0.6575), indicating an integration of diffusion and erosion processes. Furthermore, BER transferosomal gel displayed substantial anti- inflammatory activity in rats (p < 0.001). result: The independent variables exerted a substantial impact on drug entrapment and transferosome vesicle size. The optimized batch (F5) exhibited 72.11 % of BER entrapment and 77.9 nm vesicle size. DSC studies indicated molecular dispersion of BER in phospholipon G. The change in BER crystalline state was indicated by the XRD study. In vitro, diffusion study of Transferosome gel formulation indicated the sustained release by a non-fickian mechanism. Ex vivo skin permeation revealed significant improvement in BER permeation (p< 0.05). Further, the tape-stripping method revealed higher BER skin permeability. In-vivo anti-inflammatory efficacy of BER transferosome gel was significantly higher as compared to plain BER gel. Conclusion: The findings demonstrated the potential of transferosomal gel as a promising approach for efficient drug delivery and therapeutic efficacy.

Pharmacological evaluation of a new nanoformulation in the erectile tissue of rabbits and humans

The failure of achieving a penile erection for satisfactory sexual intercourse is known as erectile dysfunction (ED). The primary mediator for penile erection is nitric oxide (NO). ED is often associated with endothelial/nitrergic dysfunction characterized by a reduction of the bioavailability of NO. Phosphodiesterase-5 inhibitors (PDE-5Is) clinical efficacy in the treatment of ED depends on the integrity of the NO-sGC-PKG pathway. In the present study, we probed the effect of sodium nitroprusside incorporated into mesoporous silica nanoparticles (MPSi-NP), which traps cyanide and slowly releases NO. MPSi-NP induced a maximal relaxation of 92.8 ± 5.2% in rabbit corpora cavernosa (RbCC), blunted by a soluble guanylate cyclase (sGC) inhibitor and blockers of calcium-dependent potassium channels. MPSi-NP abolished spontaneous contractions of human corpora cavernosa (HCC) strips. In addition, MPSi-NP induced maximal relaxation of phenylephrine precontracted HCC by 118.6 ± 3.6%, and in comparison, tadalafil induced a maximal relaxation of HCC by 98.3 ± 1.2%. Similarly, the sGC inhibitor blocked the MPSi-NP relaxation. MPSi-NP potentiated the relaxation induced by tadalafil. MPSi-NP increased cGMP levels in HCC strips by 2.6-fold and increased by 3.5-fold the phosphorylation level of the VASP protein, which is a downstream target to PKG. MPSi-NP effectively relaxes RbCC and HCC by activating the sGC-PKG pathway and potentiates the tadalafil response. MPSi-NP could be helpful in conditions where nitric oxide availability is decreased. A topical gel formulation of MPSi-NP could be used as a rescue therapy to treat true non-responders of PDE5Is drugs.

Development, characterization and evaluation of in vitro safety and in vivo efficacy of repellent gel formulations

Contagious diseases caused by mosquito bites are responsible for epidemic outbreaks around the world. Applying mosquito repellents is the main and most cost-effective prophylactic measure to reduce the transmission risk of arboviruses. In this study, two topical gel Formulations were developed as mosquito repellents which use two different systems to release 20 % Icaridin. The first, Formulation 1b uses Pluronic F127®, and the second, Formulation 2b uses a biopolymer produced by bacteria from the Rhizobium tropici species. The repellent Formulations developed showed non-Newtonian behavior. For Formulation 1b the viscosity increased after adding Icaridin. However, for Formulation 2b, there was no increase in viscosity after adding the active substance. The thixotropy analysis showed that the Formulations have good recovery of their structure and adhesion. Adding of Icaridin led to an increase in gel strength in Formulation 1b and did not change the gel strength for Formulation 2b. The Formulations presented very similar occlusion capacities which were all higher than free Icaridin. The Formulations were not cytotoxic in the concentration range between 0.04 % and 0.3 %. In addition, at the 0.62 % concentration, they showed a slight reduction in cell viability, although the LD50 value was not reached. The mean protection time was longer for Formulation 2b compared to Formulation 1b. Both Formulations had a longer mean protection time than free Icaridin against Aedes aegypti. The combination of Icaridin with Pluronic F127® and the biopolymer is an innovation in the pharmaceutical area.

Application of validated size-exclusion chromatography method for physicochemical characterization of topical gel formulation of deferoxamine conjugated with PEGylated carbon nanoparticles

The focus of current research work was to develop and validate size-exclusion chromatography method and develop and evaluate gel formulation of deferoxamine conjugated with PEGylated carbon nanoparticles (DEF-PEG-CNP) for topical delivery. Size-exclusion chromatography-based method was validated as per ICH guidelines. Effect of Carbopol® 974P and Transcutol® on the nanoparticles’ permeation was studied by 3-level full factorial design of experiment. Gel formulations were characterized for viscosity, cohesive and adhesive force by texture analyzer, and drug permeation through pig ear and human skin. The analytical method was specific as no interference from solvent or excipients were observed and met preset criteria of validation with limit of quantification of 0.24 ± 0.00 μg/mL. The nanoparticles permeation, steady state flux, and retained drug were statistically (p < 0.05) affected by Carbopol® 974P and Transcutol® percentage in the gel formulations. The permeation, steady state flux, and retained nanoparticles from the gel formulations varied from 23.2 ± 2.5 % to 70.9 ± 113.3 %, 0.8 ± 0.3 to 6.6 ± 2.1 μg/cm2.h, and 5.6 ± 0.3 to 38.8 ± 8.8 µg/g, respectively. Permeation of the nanoparticles was 1.9 folds higher in pig skin compared to human skin. Immunofluorescence detected successful permeation of DEF-PEG-CNP particles into skin. In conclusion, the analytical method can quantify the nanoparticles from the gel formulation without interference, and gel formulation of the nanoparticles can permeate across the skin.

Prolonged Skin Retention of Luliconazole from SLNs Based Topical Gel Formulation Contributing to Ameliorated Antifungal Activity.

The development of effective therapy is necessary because the patients have to contend with long-termtherapy as skin fungal infections usually relapse and are hardly treated. Despite being a potent antifungal agent, luliconazole (LCZ) has certainshortcomings such as limited skin penetration, low solubility in aqueous medium, and poor skin retention. Solid Lipid Nanoparticles (SLNs) were developed using biodegradable lipids by solvent injection method and were embodied into the gel base for topical administration. After in-vitro characterizations of the formulations, molecular interactions of the drug with excipients were analyzed using in-silico studies. Ex-vivo release was determined in contrast to the pure LCZ and the commercial formulation followed by in-vivo skin localization, skin irritation index, and antifungal activity. The prepared SLNs have an average particle size of 290.7nm with no aggregation of particles and homogenous gels containing SLNs with ideal rheology and smooth texture properties were successfully prepared. The ex-vivo LCZ release from the SLN gel was lower than the commercial formulation whereas its skin deposition and skin retention were higher as accessed by CLSM studies. The drug reaching the systemic circulation and the skin irritation potential were found to be negligible. Thesolubility and drug retention in the skin were both enhanced by the development of SLNs as a carrier. Thus, SLNs offer significant advantages by delivering long lasting concentrations of LCZ at the site of infection for a complete cure of the fungal load together with skin localization of the topical antifungal drug.

Tofacitinib Citrate-Loaded Topical Gel for the Treatment of Rheumatoid Arthritis: Formulation and In-vitro-In-vivo Characterization.

This study aims to create and assess the anti-arthritic activity of tofacitinib citrate (TC) as a topical gel formulation. Using the gelling agent Carbopol 980 P, seven gel formulations were formed. The gel formulations were assessed for pH, drug content, spreadability, homogeneity, and in-vitro diffusion profile. Out of all the formulations, G7 exhibited superior release characteristics (99.1%) in comparison to the other formulations. The DSC research revealed a strong endothermal peak at 214.17°C and demonstrated an interaction with the excipients taken into consideration in this investigation. While carrying out the in-vivo study, formulation G7 successfully reduced inflammation induced by CFA. Ultimately, the optimal formulation for the “G7” can be determined &amp; successfully treats inflammation associated with arthritis. As per stability studies, it was specified that there are no such major changes in the long-term and accelerated stability testing study.

Development and Characterization of Oxiconazole Loaded Plga Nanogel.

The goal of the current study is to develop and improve polylactic co-glycolic acid (PLGA) loaded with oxiconazole nanogel for topical application. Oxiconazole Nanoprecipitation was used to create the nanoparticles method using PLGA and acetone. The point prediction method served as the foundation for the ideal oxiconazole nanoparticle composition using the Minitab®21 software, three levels two factors (32 ). The optimized composition of oxiconazole nanoparticle showed a particle size of 185 ± 0.5nm with an entrapment efficiency of 95.2 ± 0.09%. Using chitosan, a naturally occurring polymer, the ideal oxiconazole nanoparticle composition was further transformed into a gel formulation. The developed topical nano gel formulation underwent additional evaluations for antifungal, drug release, permeability, and nano gel characterization. The developed oxiconazole nanogel formulation had the ideal drug content, pH, viscosity, and spreadability. The results of the medication release and penetration investigation showed that Oxiconazole released slowly (74.06 ± 0.5%) with significantly enhanced permeation across Franz diffusion cell using membrane. The antifungal ex-vivo study and skin irritancy study of nanogel results would conclude higher activity of oxiconazole nano gel. According to the overall analysis of the data, oxiconazole nanogel is the best delivery method for treating fungal infections on the skin.

Formulation and Evaluation of Nanoparticle Loaded Hydrogel Containing Antifungal Agent for the Treatment of Onychomycosis Using Factorial Design.

SLNs are hopeful carriers for the topical delivery of antifungal drugs. This research aimed to develop a topical gel combining Efinaconazole-loaded SLNs with fluconazole to enhance the treatment of onychomycosis. The objective was to formulate a nail gel that capitalizes on the localized action and improved adherence of efinaconazole, a crucial agent in treating nail disorders like onychomycosis. The formulation utilized an alcohol-based system with specialized ingredients to ensure low surface tension and optimal wetting properties. Fluconazole, a broad-spectrum third-generation triazole antifungal, was included for its systemic and superficial antifungal activity. It works by inhibiting the formation of ergosterol, a key component of fungal cell membranes, by blocking the fungal cytochrome P-450 enzyme. The SLN-based delivery system allows for the slower release of Efinaconazole, while fluconazole diffuses more rapidly. The optimized gel formulation showed sustained drug release, with Efinaconazole releasing 32.85% of the drug by the 8th hour, compared to 74.05% for fluconazole during the same period. A stability study on the F4 formulation, which utilized Carbopol 934, was conducted according to ICH guidelines and demonstrated that the gel maintained its quality attributes, such as color, odor, homogeneity, pH, and viscosity over 6 months of testing. These results indicate that the F4 topical gel formulation is stable and suitable for long-term use.

Development of formulation and evaluation of topical micro emulsion gel loaded with terbinafine HCL micro emulsion

Fungal infections, particularly in immunocompromised patients, present significant health challenges and are often difficult to treat with conventional topical therapies due to bioavailability issues. This study explores the development of a topical gel formulation using solid lipid nanoparticles (SLNs) loaded with Terbinafine, an antifungal agent, to improve drug delivery and efficacy. SLNs were prepared by a solvent diffusion method and optimized with stearic acid and poloxamer 188. The formulation with the highest entrapment efficiency (SLN F6) exhibited 92.13% ± 0.975. The optimized SLN formulation was incorporated into a gel base containing carbopol 934, resulting in SLN gel G3 with 1.5% carbopol showing the highest drug entrapment (91.39% ± 0.187). The gel was evaluated for physicochemical properties, including viscosity (369 cP), pH (6.12 ± 0.255), and spreadability (4.5). In vitro release studies indicated controlled drug release, fitting best with the Higuchi and Korsmeyer-Peppas models. FTIR analysis confirmed no significant interactions between the drug and excipients, supporting the formulation's purity and effectiveness. Scanning electron microscopy (SEM) confirmed the spherical shape and smooth surface of the nanoparticles. This study demonstrates that Terbinafine-loaded SLNs in a topical gel formulation provide a promising approach for sustained drug delivery in treating fungal infections.

Optimization and Transfollicular Delivery of Finasteride Loaded PLGA Nanoparticles Laden Carbopol Gel for Treatment of Hair Growth Stimulation

Background: One of the frequent side effects of cancer treatment is chemotherapyinduced alopecia (CIA). The psychological discomfort of hair loss may cause patients to stop receiving chemotherapy, lowering the therapy's effectiveness. Finasteride (FNS), a JAK inhibitor, has shown tremendous promise in therapeutic uses for treating baldness. Still, systemic side effects constrained its broad use in alopecia from oral treatment and a low absorption rate at the target site— PLGA-loaded nanoparticles (NPs) for topical delivery of FNS—to overcome these issues. Methods: The nano-precipitation process was used to make FNS-NPs. The independent variables (stabiliser and polymer) were PLGA (X1), P407 (X2), and sonication time (X3). Based on the point prediction method obtainable by the Box Behnken design software, the best FNS-NPs composition was selected. Entrapment efficiency, particle size, zeta potential, and polydispersity index were used to characterize the nanoparticles. Using Carbopol as a polymer, the ideal FNS-NPs composition was further transformed into a gel formulation. The prepared topical gel formulation (FNS-NPs gel) included gel characterization, Dynamic Light Scattering (DLS), Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), invitro and in vivo studies. Results: Optimized FNS-NPs (F13) had particle sizes of 175.26±3.85 nm, 0.241±0.11 PDI, 71.04±1.35 % EE, and -33.27±0.39 surface charges. There is no interaction between the drug and the excipients, according to FTIR studies. The FNS were visible in the X-ray diffractogram enclosed in a polymer matrix. The developed FNS-NPs gel formulation shows ideal drug content, viscosity, pH, and spreadability. According to the release and permeation investigation findings, FNS released slowly (68.73±0.94%) but significantly permeated the membrane more than before. In a dose- and time-dependent manner, the produced nanoparticles considerably (p≤0.05) increased FNS delivery compared to the FNS solution. The FNS-NPs gel therapy significantly increases the quantity and size of hair follicles dose-dependently. The effectiveness of the 1% FNSNPs gel and the 2% minoxidil solution were comparable. After 72 hours, the FNS-NPs gel showed no signs of skin irritation. The outcomes, therefore, showed that the trans follicular delivery mechanism of the FNS-NPs gel might stimulate hair growth. Conclusion: These findings imply that the innovative formulation that has been developed has several beneficial properties that make it suitable for FNS dermal delivery in the treatment of alopecia areata

Formulation and Evaluation of Calendula and Lavender Oil Based Topical Antifungal Gel

Aim: Calendula officinalis and Lavendula angustifolia are traditional medicinal plants that have antifungal activity. A combination of these two plants has not been known for its activity against fungus. The present study deals with the formulation and evaluation of herbal topical Antifungal gel containing essential oils of both plants. Study Design: Proto type research design. Place and Duration of Study: Smt. R. D. Gardi Pharmacy College, Nyara- Rajkot. January 2024 to April 2024. Methodology: As 90% of skin infections are caused by Candida albicans, the antifungal activity of topical gel against this species was assessed. In this investigation, we created an antifungal herbal gel by combining carbopol 940 and other excipients with the essential oils of Calendula officinalis and Lavendula angustifolia in varying concentrations. For compatibility study, FTIR study would be done. Evaluation of Antifungal gel performed by using different tests likes, pH, Stability, Extrudability, Spreadability, Viscosity, Antifungal activity against Candida albicance, and in-vitro drug diffusion study. Results: As a result, the formulation's physiochemical characteristics, in vitro antifungal efficacy, and stability analysis (stable even after 30 days) were assessed. Every herbal gel formulation with a pH of 5–7 had favorable outcomes for physiochemical measures. Out of all the formulations, batch no 4 exhibited superior release characteristics (98 %) and zone of inhibition in comparison to the other formulated batches. The drug release profile of batch 4 showed great results. Conclusion: This is the first study on the scientific evaluation of Calendula officinalis and Lavendula angustifolia essential oil as a gel for antifungal activity. Thus this study reveals both good antifungals and in-vitro drug release; their essential oil may be formulated as Topical Gel Antifungal with satisfactory physicochemical parameters.

A Novel Approach for Pain and Inflammation Management

In search for healthy, natural pain relief options is still underway, and salicin from willow bark is a historically significant molecule. The goal of this work is to create a salicin-enriched topical gel formulation as a cutting-edge method of treating pain and inflammation. The objective of this study is to create and assess a salicin- enriched gel made from willow bark, which may be used topically to treat pain and inflammation in place of oral or synthetic drugs. Willow bark was used to extract salicin, which was then added to a topical gel base. The permeability, salicin concentration, and physical stability of the formulation were evaluated.Efficacy was evaluated through in-vitro skin permeation studies and in-vivo anti- inflammatory and analgesic models. The developed salicin- enriched gel demonstrated good physical stability and consistent release of salicin. In-vitro permeation studies indicated effective skin absorption, while in-vivo tests revealed significant reduction in inflammation and pain indicators compared to controls. The gel was well-tolerated with no adverse effects observed. The salicin-enriched gel from willow bark represents a promising topical alternative for pain and inflammation management. Its efficacy and safety profile suggest potential for further development and clinical use. Future studies focusing on larger-scale clinical trials and formulation optimization are warranted to fully establish its therapeutic value.

Topical gel formulations as potential dermal delivery carriers for green-synthesized zinc oxide nanoparticles.

This study aimed to incorporate green-synthesized zinc oxide nanoparticles (ZnO NPs), functionalized with polyethylene glycol (PEG) and linked to doxorubicin (DOX), into various topical gel formulations (hydrogel, oleogel, and bigel) to enhance their dermal delivery. The ZnO NPs were produced using the aqueous extract of the root hair of Phoenix dactylifera. The optimized green-synthesized ZnO NPs, PEGylated and conjugated to DOX, demonstrated a particle size below 100nm, low polydispersity index, and zeta potential between - 11 and - 19 mV. The UV-Vis spectroscopy analysis confirmed characteristic absorption peaks at 351 and 545nm for ZnO and DOX, respectively. The transmission electron microscope (TEM) images revealed well-dispersed spherical nanoparticles without aggregation. Additionally, ZnO NPs-loaded gels exhibited uniformity, cohesion, no phase separation, pseudoplastic flow, and viscoelastic properties. The in vitro release studies showed that DOX-PEG-ZnO NPs hydrogel released 99.5% of DOX after 5h of starting the release. Moreover, the penetration of DOX-PEG-ZnO NPs through excised rat skin was visualized by TEM. In conclusion, the hydrogel formulation containing green-synthesized DOX-PEG-ZnO NPs holds great promise for dermal administration in skin cancer treatment. Furthermore, the release rate and skin penetration of DOX from gels were varied based on the type of gel matrix and corroborated with their corresponding rheological properties.

Development of topical silver nano gel formulation of Bixin: Characterization, and evaluation of anticancer activity

ObjectiveSkin cancer refers to the pathological condition characterized by the proliferation of atypical skin cells in an uncontrolled manner. Plant-based products such as bixin although show promising anticancer properties, but maintaining their stability in a formulation is a difficult task. The objective of the research is to formulate a silver nanoparticle gel preparation of bixin and evaluate its anticancer properties. MethodsThe extract from Bixa orellana seed was prepared by hot extraction technique to isolate the active ingredient, bixin. A green synthesis approach was utilized for preparing the silver nanoparticle gel of bixin (BOAgNPs). Characterization of silver nanoparticles was done using FTIR, scanning electron microscopy, compatibility study, homogeneity testing, pH evaluation, and drug content determination. The in-vitro anticancer activity was performed using cell lines (B16F10) and in-vivo by chemical carcinogen (7,12-dimethylbenz (a) anthracene) in mice. ResultsThe BOAgNPs-loaded topical gel was found to be homogeneous (clear orange color) and pH-compatible (pH ≈ 6.66) with the skin. The characterization studies indicated the presence of all functional groups in the formulation. An optimized batch of bixin-nano gel showed about 60% inhibitory effects on B16F10 cell lines (in-vitro activity) when equated with a reference drug, 5-fluorouracil. The in-vivo anticancer study suggested suppression of tumorigenesis and promotion of the healing process with bixin-nano gel application on the skin. ConclusionThe results suggested the promising anticancer property of bixin when formulated in silver nanoparticle gel. The preparation of silver particles nano gel with bixin might provide an effective alternative option for treating skin cancers, provided more research complements the findings of the present study.

Formulation and evaluation of polyherbal topical gel for antiacne purpose

Formulation and evaluation of polyherbal topical gel for antiacne purpose

Linezolid Loaded Nanoparticle for Topical Administration of Diabetic Foot Treatment: Formulation, In Vitro and Ex Vivo Characterization

The aim of this research work was to develop a topical gel formulation containing nanoparticle to diabetic foot ulcer (DFU). In this respect, the nanoparticle formulations were prepared by using spontaneous emulsification technique. The linezolid (LZD) loaded nanoparticle formulation exhibited an low average particle size (PS) of 195.27±5.42 nm, low polydispersity index (PI) of 0.214±0.019, a high zeta potential (ZP) of 20.57±0.35 and high drug entrapment efficiency (EE) of 99.746±0.021%. In order to enhance topical residence time, the LZD-loaded nanoparticles were dispersed in a gel formulation using Methocel TM K4M (HPMC) and Carbopol® 974 P NF. The formulated gels demonstrated favorable characteristics, including an appropriate pH value, suitable mechanical performance, and desirable viscosity and spreadability for topical administration. All formulations displayed pseudoplastic flow and exhibited typical gel-type mechanical spectra at the specified frequency value. Moreover, the developed formulation achieved sustained drug release as intended for these systems. During the ex vivo drug diffusion studies, 0.007±0.004% of LZD was found in receptor phase, and this was an indicator of local effect. The optimum formulation was stable for 6 months. The initial findings suggest that the formulated topical gel containing LZD-loaded nanoparticles holds promise as an effective drug delivery system for DFU management. However, further comprehensive investigations are required to substantiate this hypothesis.

Lesson from nature: Zataria multiflora nanostructured lipid carrier topical gel formulation against Candida-associated onychomycosis, a randomized double-blind placebo-controlled clinical trial

PurposeThe increasing resistance to onychomycosis treatment globally is a major concern as it results in treatment failures. This research aimed to investigate the effectiveness of incorporating nanostructured lipid carriers (NLCs) in a gel formulation for treating mild to moderate Candida-associated onychomycosis using Zataria multiflora (Zt) essential oils. MethodsThe characteristics of Zataria multiflora-loaded nanostructured lipid carriers (Zt-NLCs) were validated using a carbopol gel (1 % w/w). In vitro tests were conducted using CLSI M60 standards to evaluate the susceptibility of ten commonly encountered dermatophyte species to antifungal agents. A clinical study was conducted involving 40 volunteers randomly assigned to two groups: one receiving the Zt-NLCs gel and the other receiving a placebo, using a double-blind, placebo-controlled design. The objective was to assess clinical manifestations and mycological findings after topical application for 2 and 4 weeks. The causative agents' species were identified using a PCR-RFLP method. ResultsThe preparation of Zt-NLCs gel resulted in a uniform suspension of spherical nanoparticles with favourable characteristics and no cytotoxic effects. Zt-NLCs demonstrated significant inhibitory effects on fungal growth and effectively improved clinical and mycological criteria in comparison to the placebo group (p < 0.005), even after 2 weeks of treatment. The C. albicans complex was recognized as the predominant species isolated from the patients using PCR-RFLP. ConclusionThe administration of Zt-NLCs gel for two weeks showed significant efficacy in disease management, as reported by both dermatologists and mycologists and therefore shows its potential use as a treatment against Candidal onychomycosis.