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Öğe Azelaic acid loaded chitosan and HPMC based hydrogels for treatment of acne: Formulation, characterization, in vitro-ex vivo evaluation(Taylor & Francis Ltd, 2022) Arpa, Muhammet Davut; Seçen, İkbal Merve; Erim, Ümit Can; Hoş, Ayşegül; Üstündağ Okur, NeslihanIn this study, hydrogels containing azelaic acid were developed using chitosan or HPMC (1-7%) for local treatment of acne vulgaris. Physicochemical properties such as viscosity, pH and mechanical properties were evaluated. In vitro release and ex vivo permeability studies were performed using the Franz diffusion cell system. The pH of the hydrogels was highly compatible with the skin pH and varied between 4.38 and 5.84. The cumulative release percentages of the hydrogels at the end of 6 hours were 65-78%, whereas the marketed product yielded 50% drug release. According to the ex vivo permeability results, azelaic acid accumulated in the skin was found to be 9.38 +/- 0.65% (marketed cream), 19.53 +/- 1.06% (K3), 10.96 +/- 1.91% (H6). The antiacne studies with Cutibacterium acnes revealed that K3 (29.45 +/- 0.95) and H6 (32.35 +/- 0.15) had higher inhibition zones compared to the marketed cream (24.50 +/- 0.90). Additionally, the gels were found to be highly stable as a result of the stability studies for 6 months. Among the hydrogels that were prepared based on experimental findings, K3 (3% Chitosan) and H6 (6% HPMC) represented elevated in vitro release profile, higher permeability and increased antiacne activity. The findings of this research suggest that the developed hydrogels might be an alternative to the marketed product.Öğe Chitosan-based buccal mucoadhesive bilayer tablets enhance the bioavailability of tizanidine hydrochloride by bypassing the first-pass metabolism(2024) Arpa, Muhammet Davut; Üstündağ Okur, Neslihan; Gök, Mehmet Koray; Cevher, ErdalTizanidine hydrochloride (TZN) is an antimuscarinic agent used in the treatment of pain-related spasms, multiple sclerosis, and stroke-related spasticity. It has low oral bioavailability (40 %) due to excessive first-pass metabolism in the liver. The aim of this project was to enhance the systemic bioavailability of TZN by developing buccal mucoadhesive bilayer tablet formulations using chitosan salts with molecular weights of 136 kDa (7 cP) and 169 kDa (10 cP). Structural characterisation of chitosans and their salts was performed by FTIR, 1H NMR, DSC, TGA, and XRD analyses. Soluble chitosan salts, chitosan glutamate and chitosan chloride, for the adhesive layer, and insoluble ethyl cellulose for the impermeable backing layer were selected as polymers to fabricate the buccal tablets by direct compression method. The tablets containing TZN demonstrated high swelling and good mucoadhesion characteristics as well as released all the drug within 8 h. While TC10, formulated with 10 cP chitosan chloride, showed the highest swelling properties, TG10, prepared with 10 cP chitosan glutamate, exhibited the highest mucoadhesion. Chitosan glutamate tablets (TG7 and TG10) demonstrated better mucoadhesive characteristics and stability than chitosan chloride ones (TC7 and TC10) in the buccal medium based on the results of swelling and drug release studies. The permeability studies performed by Franz diffusion cell demonstrated that the amount of TZN passing through the bovine buccal mucosa was between 13.4 and 14.4 %. Stability studies conducted at 5 ± 2 °C, 25 ± 2 °C and 40 ± 2 °C for 6 months showed that no changes in the content uniformity and pH were observed. The in vivo comparative bioavailability studies in female New Zealand rabbits were performed and TZN-containing buccal mucoadhesive bilayer tablets fabricated with both chloride (TC10) and glutamate (TG10) salts of chitosan demonstrated three times higher bioavailability than the commercial TZN product (Sirdalud® oral tablet) administered by the gastrointestinal route.Öğe Chitosan-based buccal mucoadhesive patches to enhance the systemic bioavailability of tizanidine(Elsevier B.V., 2023) Arpa, Muhammet Davut; Üstündağ Okur, Neslihan; Gök, Mehmet Koray; Özgümüş, Saadet; Cevher, ErdalTizanidine hydrochloride (TZN) is a muscle relaxant used to treat a variety of disorders such as painful muscle spasms and chronic spasticity. TZN has low oral bioavailability due to extensive first-pass metabolism and is used orally at a dose of 6–24 mg per day. In the present study, buccal patches were prepared by solvent casting method using chitosan glutamate (Chi-Glu) and novel chitosan azelate (Chi-Aze) which was synthesised in-house for the first time, to enhance the bioavailability of TZN by bypassing first-pass metabolism. The characterisation, mucoadhesion and drug release studies were performed. Chi-Aze patches retained their integrity longer in the buccal medium and showed higher ex vivo drug permeability compared to that prepared with Chi-Glu. In vivo studies revealed that buccal formulation fabricated with Chi-Aze (3%) showed approx 3 times more bioavailability than the orally administered commercial product. Results of the studies indicate that Chi-Aze, prepared by conjugation of chitosan and a fatty acid, the patch formulation is a promising buccal mucoadhesive system due to the physical stability in buccal medium, the good mucoadhesiveness and the high TZN bioavailability. Moreover, Chi-Aze patch might be an alternative to oral formulations of TZN to reduce the dose and frequency of drug administration.Öğe Design of IKVAV peptide/gold nanoparticle decorated, micro/nano-channeled PCL/PLGA film scaffolds for neuronal differentiation and neurite outgrowth(Elsevier Ltd, 2023) Aydeğer, Asel; Ayşit, Neşe; Baydaş, Gülsena; Çakıcı, Çağrı; Erim, Ümit Can; Arpa, Muhammet Davut; Özçiçek, İlyasIn the field of neural tissue engineering, intensive efforts are being made to develop tissue scaffolds that can support an effective functional recovery and neural development by guiding damaged axons and neurites. Micro/nano-channeled conductive biomaterials are considered a promising approach for repairing the injured neural tissues. Many studies have demonstrated that the micro/nano-channels and aligned nanofibers could guide the neurites to extend along the direction of alignment. However, an ideal biocompatible scaffold containing conductive arrays that could promote effective neural stem cell differentiation and development, and also stimulate high neurite guidance has not been fully developed. In the current study, we aimed to fabricate micro/nano-channeled polycaprolactone (PCL)/Poly-D,L-lactic-co-glycolic acid (PLGA) hybrid film scaffolds, decorate their surfaces with IKVAV pentapeptide/gold nanoparticles (AuNPs), and investigate the behavior of PC12 cells and neural stem cells (NSCs) on the developed biomaterial under static/bioreactor conditions. Here we show that channeled groups decorated with AuNPs highly promote neurite outgrowth and neuronal differentiation along linear lines in the presence of electrical stimulation, compared with the polypyrrole (PPy) coating, which has been used traditionally for many years. Hopefully, this newly developed channeled scaffold structure (PCL/PLGA-AuNPs-IKVAV) could help to support long-distance axonal regeneration and neuronal development after different neural damages.Öğe Development and evaluation of azelaic acid-cyclodextrin hydrogels for treatment of acne(Marmara University, 2024) Arpa, Muhammet Davut; Doğan, Nilay; Gündüz, Melisa; Karavelioğlu, Elçin Su; Erim, Ümit CanAcne is an inflammatory or non-inflammatory disease that can be seen at every stage of human life and affects daily life both physically and psychologically. In the topical treatment of acne, substances with different pharmacological effects such as benzoyl peroxide, isotretinoin, azelaic acid (AZE), and erythromycin are used alone or in combination. AZE cream (20%) has been frequently preferred in the treatment of mild and moderate acne in recent years. However, since AZE has poor solubility in water, its low permeability problems may occur. In this study, the soluble form of AZE was obtained by forming an inclusion complex of AZE with 2-hydroxypropyl ?-cyclodextrin (H?C). In addition, the gel formulation, which generally exhibits higher permeability properties than oily formulations, was prepared using hydroxypropyl methylcellulose (HPMC). The formation of the inclusion complex was confirmed by NMR, XRD, DSC, and FTIR analyses. As a result of the characterization studies of the hydrogel formulations, it was determined that they had pseudoplastic flow and their viscosity was approximately 220 Pa.s. In drug release studies conducted with the dialysis bag method, it was found that the AZE-H?C hydrogel formulations had a similar cumulative release percent as H?C-free hydrogels but showed a higher cumulative release percent than the commercial cream (Azelderm, Orva, Türkiye). It was proven that the drug release of the formulations that exhibit a release profile in accordance with Higuchi kinetics was different from Azelderm according to difference (f1) and similarity (f2) factors.Öğe Development and evaluation of mesoporous montmorillonite/magnetite nanocomposites loaded with 5-Fluorouracil(Elsevier, 2020) Çiftçi, Hakan; Arpa, Muhammet Davut; Gülaçar, İsmail Musab; Özcan, Levent; Ersoy, BahriPorous magnetic nanomaterials have attracted great attention in a variety of applications, particularly in the magnetically targeted and/or controlled release of various species. In this study, a new route was determined to prepare magnetic and mesoporous montmorillonite/magnetite nanocomposites (Mt-Mag NCs). The changes of textural properties of Mt-Mag NCs as a function of the surfactant and silica precursor composition ratios were investigated for the first time. The NCs were then investigated for loading and release performance of 5-Fluorouracil (5-Fu). The NCs, selected for 5-Fu loading and release studies, showed a high surface area about 340.8 m(2)/ g, an average pore diameter of 8.24 nm, and a magnetization saturation of 18.7 emu/g. Interesting new information was also obtained in the method of determining 5-Fu by UV and the method was slightly modified according to obtained results. In vitro release experiments revealed that the NCs showed sustained release profiles of 5-Fu lasting approximately 8 h. Release profiles of 5-Fu from NCs could be fitted by Korsmeyer-Peppas and Hixson kinetics. In vitro cytotoxic study using MCF7 and CRL-4010 cell lines showed that the NCs are good candidates to delivery 5-Fu.Öğe Formulation, characterization and in vitro release studies of terbinafine hydrochloride loaded buccal films(Marmara University, 2021) Arpa, Muhammet Davut; Ünükür, Melike Zeynep; Erim, Ümit CanBuccal administration of different active ingredients as an alternative to oral or dermal routes has been widely studied. The films are one of the most investigated dosage forms regarding the buccal formulations developed using bioadhesive polymers. Having thin and flexible structures, the films remain in the mouth for their duration of action without causing any discomfort. There are many studies conducted to develop buccal films for local treatment of oral fungal infections. In this research, buccal films were prepared using terbinafine hydrochloride, which is frequently used orally and systemically in the treatment of fungal infections and has low water solubility. The films were prepared by solvent casting method using hydroxypropyl methyl cellulose (HPMC) and polyvinyl pyrrolidone K30 (PVP) as the bioadhesive polymers and glycerin (2-3%) as the plasticizer. Characterization properties including thickness, weight uniformity, flexibility, tensile strength, swelling capacity were examined and the bioadhesive characteristics were determined by Texture Analyzer device using bovine buccal tissue. According to the findings of bioadhesion studies, the highest bioadhesive properties were detected in F1 and F7 formulations, which contained 5% HPMC. In vitro release studies exhibited that F1 and F7 film formulations with 5% HPMC represented slower and more controlled release compared to F2 and F8 film formulations having 4% HPMC + 1% PVP. The results revealed that the developed buccal formulations loaded with terbinafine hydrochloride might be convenient for the local treatment of oral fungal infections.Öğe New therapeutic system based on hydrogels for vaginal candidiasis management: Formulation-characterization andin vitroevaluation based on vaginal irritation and direct contact test(Taylor and Francis Ltd., 2020) Arpa, Muhammet Davut; Yoltaş, Ayşegül; Onay Tarlan, Ecehan; Şahin Şenyüz, Cemre; Sipahi, Hande; Aydın, Ahmet; Üstündağ Okur, NeslihanThe objective of the present research was to examine the possible usage of terbinafine loaded hydrogels for vaginal application as part of vaginal candidiasis treatment. Vaginal candidiasis belongs to the most frequent gynecological disorders. Various antifungal drugs are used for its treatment, with Terbinafine being one of them. In this study, new gel formulations were prepared for Terbinafine vaginal delivery. Natural polymers such as chitosan, sodium carboxymethylcellulose, and Carbopol were used for the development of Terbinafine vaginal gels. The developed gels were examined for their viscosity and spreadability, pH and mechanical properties. The most optimal formulations were further evaluated for theirin vitrorelease behavior and antifungal activities. In further, the cytotoxicity and irritation inducing capacity of optimum gel formulations were evaluated.In vitrodrug release studies demonstrated that terbinafine release was prolonged whereas anti-candida activity in several species showed the superiority of the gels compared to the marketed product. G-5 and G-8 gels did not cause lysis, hemorrhage and coagulation, therefore, classified as non-irritant. The optimal formulations were also studied for their stability, demonstrating that they were stable for 3 months.Öğe Novel benzydamine hydrochloride and chlorhexidine gluconate loaded bioadhesive films for local treatment of buccal infections(Editions de Sante, 2023) Arpa, Muhammet Davut; Yağcılar, Ayşe Pınar; Biltekin, Sevde NurBenzydamine hydrochloride (BZD), chlorhexidine gluconate (CHG) or their combination are frequently used as liquid dosage forms for the local treatment of buccal fungal and bacterial infections. However, the short residence time of liquid formulations in the oral cavity and the necessity of frequent applications limit the treatment effectiveness. To this end, CHG and BZD loaded buccal bioadhesive films, which remain at the application site longer than the liquid forms, were developed using hydroxypropyl methyl cellulose (HPMC) (2–4%) and chitosan (2–4%). The swelling studies revealed that P1, P3 and P4 films remained without loss of their integrity in the buccal medium for more than 2 h compared to other developed films. Bioadhesion studies performed with a texture analyser showed that P3 (2% chitosan+4% HPMC) yielded the greatest bioadhesion work (0.403 ± 0.027 mJ/cm2). The in vitro drug release from buccal films was evaluated by the paddle over disk method. Ex vivo penetration and permeation studies demonstrated that CHG did not pass through bovine buccal mucosa, whereas 4.82–27.35 ?g/cm2 of BZD passed through the mucosa. However, the amount of BZD and CHG accumulated in the mucosa ranged between 127.86 and 190.76 ?g/cm2 and 54.09–94.76 ?g/cm2, respectively. Additionally, both penetration and antimicrobial activity studies revealed that the buccal films were more effective than the marketed spray product. The obtained data demonstrate that the developed films are promising candidates for the buccal delivery of CHG and BZD.Öğe Novel microemulsion containing benzocaine and fusidic acid simultaneously: Formulation, characterization, and in vitro evaluation for wound healing(Springer Science and Business Media Deutschland GmbH, 2024) Arpa, Muhammet Davut; Çağlar, Emre Şefik; Güreşçi, Dilara; Sipahi, Hande; Üstündağ Okur, NeslihanModern drug carrier technologies, such as microemulsions with small droplet sizes and high surface areas, improve the ability of low water solubility active ingredients to permeate and localize. The goal of this study was to create microemulsion formulations for wound healing that contained both fusidic acid (FA), an antibacterial agent, and benzocaine (BNZ), a local anesthetic. Studies on characterization were carried out, including viscosity, droplet size, and zeta potential. The drug-loaded microemulsion had a stable structure with –3.014 ± 1.265 mV of zeta potential and 19.388 ± 0.480 nm of droplet size. In both in vitro release and ex vivo permeability studies, the microemulsion was compared with Fucidin cream and oily BNZ solution. According to the drug release studies, BNZ release from the microemulsion and the BNZ solution showed a similar profile (p > 0.05), while FA release from the microemulsion had a higher drug release compared to Fucidin cream (p < 0.001). The microemulsion presented lower drug permeation (p > 0.05) for both active ingredients, on the other hand, provided higher drug accumulation compared to the control preparations. Moreover, according to the results of in vitro wound healing activity, the microemulsion indicated a dose-dependent wound healing potential with the highest wound healing activity at the highest concentrations. To the best of our knowledge, this developed BNZ- and FA-loaded microemulsion would be a promising candidate to create new opportunities for wound healing thanks to present the active ingredients, which have low water solubility, in a single formulation and achieved higher accumulation than control preparations.Öğe Novel sprayable thermosensitive benzydamine hydrogels for topical application: Development, characterization, and in vitro biological activities(Springer Science and Business Media Deutschland GmbH, 2023) Arpa, Muhammet Davut; Kesmen, Ebrar Elif; Biltekin, Sevde NurBenzydamine hydrochloride (BZD) having analgesic, anesthetic, and anti-inflammatory effects is used orally or topically in the treatment of disorders such as joint inflammation and muscle pain. Within the scope of this study, sprayable thermosensitive BZD hydrogels were developed using thermoresponsive poloxamers to avoid systemic side effects and to provide better compliance for topical administration. Also, hydroxypropyl methyl cellulose (HPMC) was employed to improve the mechanical strength and bioadhesive properties of the hydrogel. The addition of BZD generally decreased the viscosity of the formulations (p < 0.05), while increasing the gelation temperature (p < 0.05). The formulations that did not have any clogs or leaks in the nozzle of the bottle during the spraying process were considered lead formulations. To spray the formulations easily, it was found that the viscosity at RT should be less than 200 mPa·s, and their gelation temperature should be between 26 and 34°C. Increasing HPMC and poloxamer improved bioadhesion. The amount of HPMC and poloxamers did not cause a significant change in the release characteristics of the formulations (p > 0.05); the release profiles of BZD from the formulations were similar according to model-independent kinetic (f2 > 50). HPMC and poloxamers had important roles in the accumulation of BZD in the skin. In vitro biological activity studies demonstrated that the formulations presented their anti-inflammatory activity with TNF-? inhibition but did not have any effect on the inhibition of COX enzymes as expected. As a result, thermosensitive hydrogels containing BZD might be an appropriate alternative, providing an advantage in terms of easier application compared to conventional gels. Graphical Abstract: [Figure not available: see fulltext.]Öğe Preparation and evaluation of novel microemulsion-based hydrogels for dermal delivery of benzocaine(Taylor & Francis Ltd, 2017) Üstündağ Okur, Neslihan; Çağlar, Emre Şefik; Arpa, Muhammet Davut; Karasulu, Hatice YeşimThe purpose of the current research was to prepare and evaluate the potential use of microemulsion-based hydrogel (MBH) formulations for dermal delivery of benzocaine (BZN). The pseudoternary-phase diagrams were constructed for various microemulsions composed of isopropyl myristate (IPM) as oil phase, Span 20, Tween 20, Tween 80, cremophor EL and cremophor RH40 as surfactants, ethanol as cosurfactant and distilled water as aqueous phase. Finally, concentration of BZN in microemulsions was 2% (w/w). The physicochemical properties, such as conductivity, viscosity, pH, droplet size, polydispersity index and zeta potential of microemulsions, were measured. Carbopol 940 was used to convert BZN-loaded microemulsions into gel form without affecting their structure. Furthermore, excised rat abdominal skin was used to compare permeation and penetration properties of BZN loaded M3 and M3BHs with BZN solution. According to ex vivo study results, BZN-loaded M3BH1 showed highest flux values and high release rate values, and furthermore, this gel formulation had low surfactant content. Finally, in order to learn the localization of formulations within the dermal penetration, formulations and BZN solution were labeled with red oil O and subjected to fluorescence observation. In conclusion, BZN-loaded MBHs could be offered as a promising strategy for dermal drug delivery.Öğe Sprayable microemulsion of diphenhydramine hydrochloride for dermal delivery(2024) Arpa, Muhammet Davut; Arslan, Tuğba; Eraslan, Huriye; Üstündağ Okur, NeslihanIn this work, a sprayable microemulsion of diphenhydramine hydrochloride (DPH HCl) was developed for use in conditions that cause itching, such as insect bites, mild sunburns, and skin irritations. Microemulsions were prepared using oleic acid and isopropyl myristate as the oil phase (1:2), Tween 20 and Transcutol HP as surfactants, isopropyl alcohol as co-surfactant, and water. The microemulsions (M1, M2, and M3) that presented greater area were selected as lead microemulsions and loaded with 2% DPH HCl (w/w). The physical stabilities of drug-loaded formulations with a droplet size of 15.998-19.030 nm, polydispersity index of 0.404-0.516, and turbidity of 2.41-2.50 Ntu were evaluated as appropriate. The microemulsions showed a great spread area in sprayability studies. Moreover, DPH HCl release from microemulsions reached 80-100% within one hour. The sprayable microemulsions were highly suitable for topical application of DPH HCl and can be evaluated for clinical applications with further studies.
