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The goal of the current study was to explore the potential benefits of Acitretin (Act) nanovesicular gel as a prospective antipsoriatic topical delivery system counteracting the drug challenges in terms of its extremely low aqueous solubility, instability, skin irritation, and serious systemic adverse effects. Act-loaded niosomes were successfully developed, entirely characterized, and optimized. Further evaluation of the optimized formula was conducted regarding its stability and ex vivo cytotoxicity on different cell lines. The optimized niosomal vesicles were then incorporated in gel base matrix and investigated by sequential ex vivo (skin permeation and deposition) and in vivo (skin irritation and antipsoriatic activity using mouse tail model) experiments. The optimized Act-loaded niosomes (span 60:cholesterol molar ratio 1:1) were spherical in shape and exhibited the highest entrapment efficiency (90.32±3.80%) with appropriate nanosize and zeta potential of 369.73±45.45 nm and -36.33±1.80 mV, respectively. Encapsulation of the drug in the nanovesicles was further emphasized by differential scanning calorimetric and powder X-ray diffraction studies. After 3 months storage at 4±1°C, the optimized formula preserved its stability. Act nano niosomal gel produced a remarkable enhanced ex vivo permeation profile up to 30 h and significant drug deposition in the viable epidermal-dermal layers compared with those of Act gel. The pronounced antipsoriatic activity of the medicated nano niosomes was proved ex vivo in HaCaT cells (a keratinocyte cell line). Topical application of Act nano niosomal gel to mouse tail model further established its distinct in vivo antipsoriatic superiority in terms of significantly higher orthokeratosis, drug activity, and reduction in epidermal thickness compared with the control and other gel formulations. Also, negligible skin irritation and better skin tolerability of Act nanovesicular gel were revealed by primary irritation index and histopathologic examination.

Naringin is one of the most interesting phytopharmaceuticals that has been widely investigated for various biological actions. Yet, its low water solubility, limited permeability, and suboptimal bioavailability limited its use. Therefore, in this study, polymeric micelles of naringin based on pluronic F68 (PF68) were developed, fully characterized, and optimized. The optimized formula was investigated regarding in vitro release, storage stability, and in vitro cytotoxicity vs different cell lines. Also, cytoprotection against ethanol-induced ulcer in rats and antitumor activity against Ehrlich ascites carcinoma in mice were investigated. Nanoscopic and nearly spherical 1:50 micelles with the mean diameter of 74.80±6.56 nm and narrow size distribution were obtained. These micelles showed the highest entrapment efficiency (EE%; 96.14±2.29). The micelles exhibited prolonged release up to 48 vs 10 h for free naringin. The stability of micelles was confirmed by insignificant changes in drug entrapment, particle size, and retention (%) (91.99±3.24). At lower dose than free naringin, effective cytoprotection of 1:50 micelles against ethanol-induced ulcer in rat model has been indicated by significant reduction in mucosal damage, gastric level of malondialdehyde, gastric expression of tumor necrosis factor-alpha, caspase-3, nuclear factor kappa-light-chain-enhancer of activated B cells, and interleukin-6 with the elevation of gastric reduced glutathione and superoxide dismutase when compared with the positive control group. As well, these micelles provoked pronounced antitumor activity assessed by potentiated in vitro cytotoxicity particularly against colorectal carcinoma cells and tumor growth inhibition when compared with free naringin. In conclusion, 1:50 naringin-PF68 micelles can be represented as a potential stable nanodrug delivery system with prolonged release and enhanced antiulcer as well as antitumor activities.

Clove essential oil is a phytochemical possessing a vast array of biological activities. Nevertheless, fabricating nano topical delivery systems targeted to augment the anti-inflammatory activity of the oil has not been investigated so far. Accordingly, in this study, controlled release nanoparticulate systems, namely nanoemulgel and nanofibers (NFs), of the oil were developed to achieve such goal. The nanoemulsion was incorporated in the hydrogel matrix of mixed biopolymers - chitosan, guar gum and gum acacia - to formulate nanoemulsion-based nanoemulgel. Taguchi's model was adopted to evaluate the effect of independently controlled parameters, namely, the concentration of chitosan (X ), guar gum (X ), and gum acacia (X ) on different dependently measured parameters. Additionally, the nanoemulsion-based NFs were prepared by the electrospinning technique using polyvinyl alcohol (PVA) polymer. Extensive in vitro, ex vivo and in vivo evaluations of the aforementioned formulae were conducted. Both Fourier transform-infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) established the complete dispersion of the nanoemulsion in the polymeric matrices of the prepared nanoemulgel and NFs. The ex vivo skin permeation data of clove essential oil from the prepared formulations showed that NFs can sustain its penetration through the skin comparably with nanoemulgel. Topical treatment with NFs (once application) and nanoemulgel (twice application) evoked a marvelous in vivo anti-inflammatory activity against croton oil-induced mouse skin inflammation model when compared with pure clove essential oil along with relatively higher efficacy of medicated NFs than that of medicated nanoemulgel. Such prominent anti-inflammatory activity was affirmed by histopathological and immunohistochemical examinations. These results indicated that nanoemulsion-based nanoemulgel and nanoemulsion-based NFs could be introduced to the phytomedicine field as promising topical delivery systems for effective treatment of inflammatory diseases instead of nonsteroidal anti-inflammatory drugs that possess adverse effects.

Apocynin (APO) is a bioactive phytochemical with prominent anti-inflammatory and anti-oxidant activities. Designing a nano-delivery system targeted to potentiate the gastric antiulcerogenic activity of APO has not been investigated yet. Chitosan oligosaccharide (COS) is a low molecular weight chitosan and its oral nanoparticulate system for potentiating the antiulcerogenic activity of the loaded APO has been described here.  COS-nanoparticles (NP ) loaded with APO (using tripolyphosphate [TPP] as a cross-linker) were prepared by ionic gelation method and fully characterized. The chosen formula was extensively evaluated regarding in vitro release profile, kinetic analysis, and stability at refrigerated and room temperatures. Ultimately, the in vivo antiulcerogenic activity against ketoprofen (KP)-induced gastric ulceration in rats was assessed by macroscopic parameters including Paul's index and antiulcerogenic activity, histopathological examination, immunohistochemical (IHC) evaluation of cyclooxygenase-2 (COX-2) expression level in ulcerated gastric tissue, and biochemical measurement of oxidative stress markers and nitric oxide (NO) levels. The selected NP formula with COS (0.5 % w/v) and TPP (0.1% w/v) was the most appropriate one with drug entrapment efficiency percentage of 35.06%, particle size of 436.20 nm, zeta potential of +38.20 mV, and mucoadhesive strength of 51.22%. It exhibited a biphasic in vitro release pattern as well as high stability at refrigerated temperature for a 6-month storage period. APO-loaded COS-NP provoked marvelous antiulcerogenic activity against KP-induced gastric ulceration in rats compared with free APO treated group, which was emphasized by histopathological, IHC, and biochemical studies.  In conclusion, APO-loaded COS-NP could be considered as a promising oral phytopharmaceutical nanoparticulate system for management of gastric ulceration.

Recently, Apocynin (APO) has emerged as a bioactive phytochemical with potent antioxidant and anti-inflammatory properties. No reports have been published so far concerning its topical application as a pharmaceutical dosage form for prospective use. To the best of our knowledge, this is the first study to fabricate novel anti-inflammatory film for external medication with APO. APO film was prepared using casein (CAS) as a natural protein film former by solvent casting technique. The medicated film was extensively evaluated in terms of its various physicochemical characteristics, ex vivo skin permeation profile, stability, and finally in vivo anti-inflammatory activity on carrageenan-induced rat paw edema. The film represented satisfactory mechanical properties along with good flexibility. Fourier transform-infrared spectroscopy, differential scanning calorimetry, and X-ray diffractometry revealed possible solubility of APO in the amorphous CAS and inter- and intramolecular hydrogen bonding between the film components. The ex vivo skin permeation results of the medicated film demonstrated non-Fickian diffusion mechanism of the permeated drug. Application of APO film to rat paw before carrageenan-induced paw edema or after induction disclosed eminent anti-inflammatory activity expressed by marked decrease in paw swelling (%) and increase in edema inhibition rate (%). In addition, histopathologic examination revealed a significant decrease in inflammatory scores. The immunohistochemical expression levels of both nuclear factor kappa B and cyclooxygenase-2 were significantly suppressed. These results indicated that CAS film could be applied as a promising external delivery system for the anti-inflammatory APO.

Tacrolimus (FK506) is a potent immunosuppressive agent widely employed to prevent allogeneic rejection in transplant recipients. However, its nephrotoxic effects pose significant limitations to long-term therapeutic use. To address this challenge, the present study aims to develop an innovative oral nano-delivery system designed to mitigate FK506-induced nephrotoxicity through the antioxidant properties of Apocynin (APO), clove oil (CO), and chitin oligosaccharide (CTOS). A nanostructured lipid carrier (NSLC) incorporating APO dissolved in CO and functionalized with CTOS was formulated using ultrasonic emulsification. Gelucire 43/01 and CO served as key lipid components in varying ratios. Physicochemical characterization of the developed NSLCs was conducted, assessing particle size (PS), polydispersity index (PDI), zeta potential (ZP), and encapsulation efficiency (EE%). The optimized formulation (F4) exhibited an EE% of 63.85 ± 1.98, PS of 123 ± 2.21 nm, PDI of 0.17 ± 0.09, and ZP of − 28 ± 1.98, demonstrating a biphasic release profile and stability under refrigerated conditions for six months. In vivo nephroprotective efficacy was evaluated in FK506-induced acute kidney injury (AKI) rat models, where oral administration of APO-loaded NSLCs significantly improved renal function and alleviated nephrotoxicity, as evidenced by biochemical markers and histopathological analyses. These findings underscore the potential of APO-loaded NSLCs as a promising oral phytopharmaceutical strategy for mitigating FK506-associated nephrotoxicity and enhancing therapeutic outcomes in transplant patients. Further studies are warranted to optimize and expand clinical applications.

Fisetin (FST) is a naturally occurring flavonol that has recently emerged as a bioactive phytochemical with an impressive array of biological activities. To the author knowledge, boosting the activity of FST against severe acute pancreatitis (SAP) through a nanostructured delivery system (Nanophytomedicine) has not been achieved before. Thereupon, FST-loaded lipid polymer hybrid nanoparticles (FST-loaded LPHNPs) were prepared through conjoined ultrasonication and double emulsion (w/o/w) techniques. Comprehensive in vitro and in vivo evaluations were conducted. The optimized nanoparticle formula displayed a high entrapment efficiency % of 61.76 ± 1.254%, high loading capacity % of 32.18 ± 0.734, low particle size of 125.39 ± 0.924 nm, low particle size distribution of 0.357 ± 0.012, high zeta potential of + 30.16 ± 1.416 mV, and high mucoadhesive strength of 35.64 ± 0.548%. In addition, it exhibited a sustained in vitro release pattern of FST. In the in vivo study, oral pre-treatment of FST-loaded LPHNPs protected against l -arginine induced SAP and multiple organ injuries in rats compared to both FST alone and plain LPHNPs, as well as the untreated group, proven by both biochemical studies, that included both amylase and lipase activities, and histochemical studies of pancreas, liver, kidney and lungs. Therefore, the study could conclude the potential efficacy of the novel phytopharmaceutical delivery system of FST as a prophylactic regimen for SAP and consequently, associated multiple organ injuries.

Apocynin (APO), a well-known bioactive plant-based phenolic phytochemical with renowned anti-inflammatory and antioxidant pharmacological activities, has recently emerged as a specific nicotinamide adenine dinucleotide phosphate-oxidase (NADPH) oxidase inhibitor. As far as we know, no information has been issued yet regarding its topical application as a nanostructured-based delivery system. Herein, APO-loaded Compritol ® 888 ATO (lipid)/chitosan (polymer) hybrid nanoparticles (APO-loaded CPT/CS hybrid NPs) were successfully developed, characterized, and optimized, adopting a fully randomized design (3 2 ) with two independent active parameters (IAPs), namely, CPT amount (X A ) and Pluronic ® F-68 (PF-68) concentration (X B ), at three levels. Further in vitro–ex vivo investigation of the optimized formulation was performed before its incorporation into a gel base matrix to prolong its residence time with consequent therapeutic efficacy enhancement. Subsequently, scrupulous ex vivo–in vivo evaluations of APO-hybrid NPs-based gel (containing the optimized formulation) to scout out its momentous activity as a topical nanostructured system for beneficial remedy of rheumatoid arthritis (RA) were performed. Imperatively, the results support an anticipated effectual therapeutic activity of the APO-hybrid NPs-based gel formulation against Complete Freund’s Adjuvant-induced rheumatoid arthritis (CFA-induced RA) in rats. In conclusion, APO-hybrid NPs-based gel could be considered a promising topical nanostructured system to break new ground for phytopharmaceutical medical involvement in inflammatory-dependent ailments. Graphical Abstract

Apocynin (APO) is a naturally occurring acetophenone with eminent anti-inflammatory and anti-oxidant peculiarities. It suffers from poor bioavailability due to low aqueous solubility. Herein, APO was loaded in a Clove oil (CO) based Nanostructured lipid carrier (NSLC) system using a simple method (ultrasonic emulsification) guided by a quality-by-design approach (2 3 full factorial design) to optimize the formulated NSLCs. The prepared NSLCs were evaluated regarding particle size (PS), polydispersity index (PDI), zeta potential (ZP), and entrapment efficiency (EE%). The optimal formula (F2) was extensively investigated through transmission electron microscope (TEM), Fourier transform infrared (FT-IR) spectroscopy, Differential scanning calorimetry (DSC), X-ray diffractometry (XRD), in vitro release, and stability studies. Cytotoxicity against human urinary bladder carcinoma (T24) cell line and in vivo activity studies in rats with induced cystitis were also assessed. The results disclosed that the optimal formula (F2) had PS of 214.8 ± 5.8 nm with EE% of 79.3 ± 0.9%. F2 also exhibited a strong cytotoxic effect toward the T24 cancer cells expressed by IC50 value of 5.8 ± 1.3 µg/mL. Pretreatment with the optimal formula (orally) hinted uroprotective effect against cyclophosphamide (CP)-induced hemorrhagic cystitis (HC) in rat models, emphasized by histopathological, immunohistochemical, and biochemical investigations. In consideration of the simple fabrication process, APO-loaded CO-based NSLCs can hold prospective potential in the prophylaxis of oncologic and urologic diseases.

Eudragit E (EE)-sodium alginate (SA) polyelectrolyte complexes (PECs) were prepared at pH 4 and 5.8 using sodium alginate of high (SAH) and low viscosity (SAL). The optimum EE-SA complexation mass ratio was determined using viscosity measurements. Interactions between EE and SA in PECs were characterized by Fourier transform infra-red spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Diltiazem hydrochloride (DTZ HCl) tablets were prepared using the prepared EE-SA PECs and their physical mixtures at different ratios as matrices. Tablets were evaluated for swelling characteristics and in vitro drug release. Tablets containing EE-SAH physical mixtures of ratios (1.5:1 and 1:3) as matrices were effective in achieving sustained release of DTZ HCl, where the percent drug released was significantly (p < 0.05) decreased compared to that from tablets either containing the same ratios of EE-SAL physical mixtures or the preformed EE- -SAH and EE-SAL PECs.