scholarly journals Thymoquinone Loaded Topical Nanoemulgel for Wound Healing: Formulation Design and In-Vivo Evaluation

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3863
Author(s):  
Mohammed S. Algahtani ◽  
Mohammad Zaki Ahmad ◽  
Ibrahim Ahmed Shaikh ◽  
Basel A. Abdel-Wahab ◽  
Ihab Hamed Nourein ◽  
...  
Keyword(s):  
Wound Healing ◽  
Droplet Size ◽  
Therapeutic Efficacy ◽  
Drug Loading ◽  
High Energy ◽  
Polydispersity Index ◽  
Skin Permeability ◽  
Process Conditions ◽  
The Mean ◽  
Hydrogel System

Thymoquinone is a natural bioactive with significant therapeutic activity against multiple ailments including wound healing. The poor aqueous solubility and low skin permeability limit its therapeutic efficacy. The present investigation aimed to improve the biopharmaceutical attributes of thymoquinone to enhance its topical efficacy in wound healing. A nanoemulsion-based hydrogel system was designed and characterized as a nanotechnology-mediated drug delivery approach to improve the therapeutic efficacy of thymoquinone, utilizing a high-energy emulsification technique. The black seed oil, as a natural home of thymoquinone, was utilized to improve the drug loading capacity of the developed nanoemulsion system and reduced the oil droplet size to <100 nm through ultrasonication. The influence of formulation composition, and the ultrasonication process conditions, were investigated on the mean globule size and polydispersity index of the generated nanoemulsion. Irrespective of surfactant/co-surfactant ratio and % concentration of surfactant/co-surfactant mixture, the ultrasonication time had a significant (p < 0.05) influence on the mean droplet size and polydispersity index of the generated nanoemulsion. The developed nanoemulgel system of thymoquinone demonstrated the pseudoplastic behavior with thixotropic properties, and this behavior is desirable for topical application. The nanoemulgel system of thymoquinone exhibited significant enhancement (p < 0.05) in skin penetrability and deposition characteristics after topical administration compared to the conventional hydrogel system. The developed nanoemulgel system of thymoquinone exhibited quicker and early healing in wounded Wistar rats compared to the conventional hydrogel of thymoquinone, while showing comparable healing efficacy with respect to marketed silver sulfadiazine (1%) cream. Furthermore, histopathology analysis of animals treated with a developed formulation system demonstrated the formation of the thick epidermal layer, papillary dermis along with the presence of extensive and organized collagen fibers in newly healed tissues. The outcome of this investigation signifies that topical delivery of thymoquinone through nanoemulgel system is a promising candidate which accelerates the process of wound healing in preclinical study.

scholarly journals Preparation and Characterization of Curcumin Nanoemulgel Utilizing Ultrasonication Technique for Wound Healing: In Vitro, Ex Vivo, and In Vivo Evaluation

Gels ◽  
2021 ◽  
Vol 7 (4) ◽  
pp. 213
Author(s):  
Mohammed S. Algahtani ◽  
Mohammad Zaki Ahmad ◽  
Ihab Hamed Nourein ◽  
Hassan A. Albarqi ◽  
Hamad S. Alyami ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Wound Healing ◽  
Droplet Size ◽  
Topical Application ◽  
Therapeutic Efficacy ◽  
Healing Process ◽  
High Energy ◽  
The Impact ◽  
Hydrogel System

Hydrogels being a drug delivery system has great significance particularly for topical application in cutaneous open wound. Its specific physicochemical properties such as non-adhesiveness, moisture retention, exudate absorption, and gas permeability make them ideal as a drug delivery vehicle for wound healing application. Further, curcumin (a natural bioactive) was selected as a therapeutic agent to incorporate into the hydrogel system to design and develop nanogel pharmaceutical products for wound healing. Although, curcumin possesses remarkable anti-inflammatory, antioxidant, and anti-infective activity along with hastening the healing process by acting over the different stages of the wound healing process, but its poor biopharmaceutical (low aqueous solubility and skin penetrability) attributes hamper their therapeutic efficacy for skin applications. The current investigation aimed to develop the curcumin-loaded nanogel system and evaluated to check the improvement in the therapeutic efficacy of curcumin through a nanomedicine-based approach for wound healing activity in Wistar rats. The curcumin was enclosed inside the nanoemulsion system prepared through a high-energy ultrasonic emulsification technique at a minimum concentration of surfactant required to nanoemulsify the curcumin-loaded oil system (Labrafac PG) having droplet size 56.25 ± 0.69 nm with polydispersity index 0.05 ± 0.01 and negatively surface charge with zeta potential −20.26 ± 0.65 mV. It was observed that the impact of Smix (surfactant/co-surfactant mixture) ratio on droplet size of generated nanoemulsion is more pronounced at lower Smix concentration (25%) compared to the higher Smix concentration (30%). The optimized curcumin-loaded nanoemulsion was incorporated into a 0.5% Carbopol® 940 hydrogel system for topical application. The developed curcumin nanoemulgel exhibited thixotropic rheological behavior and a significant (p < 0.05) increase in skin penetrability characteristics compared to curcumin dispersed in conventional hydrogel system. The in vivo wound healing efficacy study and histological examination of healed tissue specimen further signify the role of the nanomedicine-based approach to improve the biopharmaceutical attributes of curcumin.

scholarly journals Nanoemulgel for Improved Topical Delivery of Retinyl Palmitate: Formulation Design and Stability Evaluation

Nanomaterials ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 848 ◽  
Author(s):  
Mohammed S. Algahtani ◽  
Mohammad Zaki Ahmad ◽  
Javed Ahmad
Keyword(s):  
Droplet Size ◽  
Delivery System ◽  
Skin Irritation ◽  
Topical Delivery ◽  
Skin Aging ◽  
Retinyl Palmitate ◽  
Skin Permeability ◽  
Therapeutic Benefits ◽  
Behavior Study ◽  
Hydrogel System

Retinyl palmitate is a vitamin A ester belonging to the family of endogenous natural retinoid and used to treat various skin disorders like acne, skin aging, wrinkles, and dark spots, as well as to protect against psoriasis. Despite the known therapeutic benefits of retinyl palmitate, the conventional topical delivery of retinyl palmitate commonly associated with adverse reactions such as skin irritation, redness, excessive peeling, and dryness. Therefore, the current study aims to encapsulate the retinyl palmitate in nanoemulsion then incorporate it into a hydrogel system to improve the topical delivery and stability. Low-energy emulsification method was used for the nano-encapsulation of retinyl palmitate. The phase behavior study was used for the investigation and the optimization of the formulation. The droplet size of the optimized nanoemulsion was in nano dimension (16.71 nm) with low polydispersity index (PdI) (0.015), negative zeta potential (−20.6 mV). It demonstrated the influence of vortexing on droplet size and PdI during nanoemulsion preparation. The retinyl palmitate loaded nanoemulgel delivery system exhibited significant improvement (p < 0.05) in skin permeability after topical application. Employment of the nano-encapsulation approach afterward dispersion into hydrogel system for the development of a topical delivery system of retinyl palmitate resulted in improvement in its UV and storage stability as well.

scholarly journals INVESTIGATION AND OPTIMIZATION OF FORMULATION PARAMETERS FOR SELFNANOEMULSIFYING DELIVERY SYSTEM OF TWO LIPOPHILIC AND GASTROINTESTINAL LABILE DRUGS USING BOX-BEHNKEN DESIGN

2018 ◽  
Vol 11 (14) ◽  
pp. 12 ◽  
Author(s):  
Bimlesh Kumar ◽  
Varun Garg ◽  
Amarjeet Singh ◽  
Narendra Kumar Pandey ◽  
Saurabh Singh ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Droplet Size ◽  
Castor Oil ◽  
Drug Loading ◽  
Research Work ◽  
Tween 80 ◽  
Box Behnken Design ◽  
The Mean ◽  
Formulation Parameters ◽  
Formula Composition

Objective: Present research work aims toward codelivery of two hydrophobic drugs, curcumin (CRM) and duloxetine hydrochloride (DXH) through self-nanoemulsifying drug delivery systems (SNEDDS).Methods: Initially, binary mixture in the ratio of 1:1 was prepared and then loaded into SNEDDS. Box-Behnken design (BBD) was adopted to develop SNEDDS. As per the optimal design, 13 SNEDDS prototypes were prepared. Castor oil, tween-80 and Transcutol P® were used as oil, surfactant, and cosurfactant, respectively. To 1 mL of SNEDDS, 30 mg each of CRM and DXH was loaded (CRM-DXH- SNEDDS).Results: The design revealed that for mean droplet size, polydispersity index (PDI), as well as percentage drug loading, all the three factors, i.e. ratio of oil (a), surfactant (b), and cosurfactant (c) were found to give significant effect. Factor B showed the most significant effect on mean droplet size (y1). In case of PDI (y2), factors B and C exerted maximum influence, whereas, Factor A has shown non-significant effect. For percentage drug loading of drugs (y3 and y4), all the three factors were found to have the most significant effect. The optimized batch of CRM-DXH- SNEDDS having composition castor oil, tween-80, and Transcutol P® in the ratio: 2.17:5.22:2.61, revealed that the mean drug loading (%) of CRM and DXH in an optimized batch of SNEDDS was found to be 87.22±1.87 and 92.32±0.19%, respectively. The mean droplet size, PDI, and zeta potential of formed SNEDDS were observed as 113.14±1.14 nm, 0.20±0.026, and −13.2 mV, respectively.Conclusion: BBD provided optimal formula composition for SNEDDS for obtaining desirable drug loading, emulsion droplet size, and zeta potential.

scholarly journals Transdermal Delivery of Snakehead Fish (Ophiocephalus striatus) Nanoemulgel Containing Hydrophobic Powder for Burn Wound

2018 ◽  
Vol 24 (4) ◽  
pp. 313-323 ◽  
Author(s):  
Robert Tungadi ◽  
Widy Susanty ◽  
Prisca Wicita ◽  
Elvira Pido
Keyword(s):  
Wound Healing ◽  
Zeta Potential ◽  
Droplet Size ◽  
Transdermal Delivery ◽  
Skin Irritation ◽  
Polydispersity Index ◽  
Gelling Agent ◽  
Burn Wound ◽  
Snake Skin ◽  
Burn Wound Healing

Background: The aim of the present study was to characterize and evaluate the nanoemulgel (NEG) of snakehead fish powder (SFP), as a transdermal delivery system for poorly water soluble drug, in order to conquer the inconveniences related to its oral conveyance. Methods: Diverse nanoemulsion components (oil, surfactant, and co-surfactant) were chosen based on solvency and emulsification capacity. SFP loaded nanoemulsion which tested by stress-stability testing was carried out for all formulations and those that passed these tests were characterized for mean droplet size, polydispersity index (PDI), zeta potential, pH, viscosity, and transmittance. After that, this was continued by permeation studies using snake skin in vitro and rabbit skin in vivo studies i.e. skin irritation study and the effectiveness test. Results: Mean droplet size and zeta potential of the optimized nanoemulsion (NE4) were found to be 98.6 ± 0.93 nm (polydispersity index, PDI = 0.1 ± 0.20) and -57.5 ± 0.3 mV respectively. Optimized nanoemulsion was converted into nanoemulgel with 1.5% w/v of gelling agent (HPMC) and evaluated for pH, viscosity, spreadability, and extrudability measurement. Ex vivo transdermal permeation value for SFP through snake skin as membrane from NEG1, NEG2, NEG3 and marketed SFP cream showed results of 55.65 ± 0.93%, 56.14 ± 0.70%, 66.75 ± 1.03% and 49.80 ± 3.42% respectively in 3 hours. Moreover, all the treatment group did not show skin irritation of each group. The effect of burn wound healing of NEG3 showed a significant (P<0.05) on the measurement of wound area compared to marketed cream. Conclusion: The novel NEG of SFP was successfully formulated for transdermal application based on the results of evaluations and stability tests on accelerating burn wound healing.

Anisotropy of damage productions in electron irradiated molybdenum

1978 ◽  
Vol 36 (1) ◽  
pp. 354-355
Author(s):  
K. Izui ◽  
S. Furuno ◽  
H. Otsu ◽  
T. Nishida ◽  
H. Maeta
Keyword(s):  
Electron Flux ◽  
Threshold Energy ◽  
High Energy ◽  
Voltage Electron ◽  
High Voltage Electron Microscope ◽  
Displacement Threshold ◽  
The Mean ◽  
Channeling Effect ◽  
Different Origins ◽  
Threshold Energies

Anisotropy of damage productions in crystals due to high energy electron bombardment are caused from two different origins. One is an anisotropic displacement threshold energy, and the other is an anisotropic distribution of electron flux near the atomic rows in crystals due to the electron channeling effect. By the n-beam dynamical calculations for germanium and molybdenum we have shown that electron flux at the atomic positions are from ∽4 to ∽7 times larger than the mean incident flux for the principal zone axis directions of incident 1 MeV electron beams, and concluded that such a locally increased electron flux results in an enhanced damage production. The present paper reports the experimental evidence for the enhanced damage production due to the locally increased electron flux and also the results of measurements of the displacement threshold energies for the <100>,<110> and <111> directions in molybdenum crystals by using a high voltage electron microscope.

Novel Formulation Development and Evaluation of Nanoparticles Based in Situ Gelling System for The Ophthalmic Delivery of Ciprofloxacin Hydrochloride

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Loading ◽  
In Vitro Release ◽  
Formulation Development ◽  
Ciprofloxacin Hydrochloride ◽  
Potential Value ◽  
The Mean ◽  
In Situ Gelling

Ciprofloxacin hydrochloride loaded Eudragit RS100 nanoparticles were prepared by using w/o/w emulsification (multiple emulsification) solvent evaporation followed by drying of nanoparticles at 50°C. The nanoparticles were further incorporated into the pH-triggered in situ gel forming system which was prepared using Carbopol 940 in combination with HPMC as viscosifying agent. The developed nanoparticles was evaluated for particle size, zeta potential value and loading efficiency; nanoparticle incorporated in situ gelling system was evaluated for pH, clarity, gelling strength, rheological studies, in-vitro release studies and ex-vivo precorneal permeation studies. The nanopaticle showed the mean particle size varying between 263.5nm - 325.9 nm with the mean zeta potential value of -5.91 mV to -8.13 mV and drug loading capacity varied individually between 72.50% to 98.70% w/w. The formulation was clear with no suspended particles, showed good gelling properties. The gelling was quick and remained for longer time period. The developed formulation was therapeutically efficacious, stable and non-irritant. It provided the sustained release of drug over a period of 8-10 hours.

The Effect of Phase Transition Temperature on Therapeutic Efficacy of Liposomal Bortezomib

2020 ◽  
Vol 20 (6) ◽  
pp. 700-708
Author(s):  
Mitra Korani ◽  
Sara Nikoofal-Sahlabadi ◽  
Amin R. Nikpoor ◽  
Solmaz Ghaffari ◽  
Hossein Attar ◽  
...  
Keyword(s):  
Side Effects ◽  
Cell Line ◽  
Therapeutic Efficacy ◽  
Drug Loading ◽  
Particle Diameter ◽  
In Vitro Cytotoxicity ◽  
Liposomal Formulations ◽  
Cytotoxicity Studies ◽  
Anti Tumor Activity

Aims: Here, three liposomal formulations of DPPC/DPPG/Chol/DSPE-mPEG2000 (F1), DPPC/DPPG/Chol (F2) and HSPC/DPPG/Chol/DSPE-mPEG2000 (F3) encapsulating BTZ were prepared and characterized in terms of their size, surface charge, drug loading, and release profile. Mannitol was used as a trapping agent to entrap the BTZ inside the liposomal core. The cytotoxicity and anti-tumor activity of formulations were investigated in vitro and in vivo in mice bearing tumor. Background: Bortezomib (BTZ) is an FDA approved proteasome inhibitor for the treatment of mantle cell lymphoma and multiple myeloma. The low solubility of BTZ has been responsible for the several side effects and low therapeutic efficacy of the drug. Encapsulating BTZ in a nano drug delivery system; helps overcome such issues. Among NDDSs, liposomes are promising diagnostic and therapeutic delivery vehicles in cancer treatment. Objective: Evaluating anti-tumor activity of bortezomib liposomal formulations. Methods: Data prompted us to design and develop three different liposomal formulations of BTZ based on Tm parameter, which determines liposomal stiffness. DPPC (Tm 41°C) and HSPC (Tm 55°C) lipids were chosen as variables associated with liposome rigidity. In vitro cytotoxicity assay was then carried out for the three designed liposomal formulations on C26 and B16F0, which are the colon and melanoma cancer mouse-cell lines, respectively. NIH 3T3 mouse embryonic fibroblast cell line was also used as a normal cell line. The therapeutic efficacy of these formulations was further assessed in mice tumor models. Result: MBTZ were successfully encapsulated into all the three liposomal formulations with a high entrapment efficacy of 60, 64, and 84% for F1, F2, and F3, respectively. The findings showed that liposomes mean particle diameter ranged from 103.4 to 146.8nm. In vitro cytotoxicity studies showed that liposomal-BTZ formulations had higher IC50 value in comparison to free BTZ. F2-liposomes with DPPC, having lower Tm of 41°C, showed much higher anti-tumor efficacy in mice models of C26 and B16F0 tumors compared to F3-HSPC liposomes with a Tm of 55°C. F2 formulation also enhanced mice survival compared with untreated groups, either in BALB/c or in C57BL/6 mice. Conclusion: Our findings indicated that F2-DPPC-liposomal formulations prepared with Tm close to body temperature seem to be effective in reducing the side effects and increasing the therapeutic efficacy of BTZ and merits further investigation.

scholarly journals The Surgical Outcomes of Unstable Ankle Fractures in Patients Aged >65 Years

2021 ◽  
Vol 12 ◽  
pp. 215145932199776
Author(s):  
Adem Sahin ◽  
Anıl Agar ◽  
Deniz Gulabi ◽  
Cemil Erturk
Keyword(s):  
Surgical Outcomes ◽  
External Rotation ◽  
High Energy ◽  
Ankle Fractures ◽  
Medial Malleolus ◽  
Aofas Score ◽  
Non Union ◽  
The Mean ◽  
Medial Malleolus Fracture ◽  
Mechanism Of Trauma

Aim: To evaluate the surgical outcomes and complications of patients over 65 years of age, with unstable ankle fractures. Material and Method: The study included 111 patients (73F/38 M) operated on between January 2015 and February 2019 and followed up for a mean of 21.2 months (range, 6-62 months).Demographic characteristics, comorbidities, fracture type, and mechanisms of injury were evaluated. Relationships between postoperative complications and comorbidities were examined. In the postoperative functional evaluations, the AOFAS score was used and pre and postoperative mobilization (eg, use of assistive devices) was assessed. Results: The mean age of the patients was 70.5 ± 6.1 years (range, 65-90 years). The mechanism of trauma was low-energy trauma in 90.1% of the fractures and high-energy trauma in 9.9%. The fractures were formed with a SER injury (supination external rotation) in 83.7% of cases and bimalleolar fractures were seen most frequently (85/111, 76%).Complications developed in 16 (14.4%) patients and a second operation was performed in 11 (9.9%) patients with complications. Plate was removed and debridement was performed in 5 of 6 patients due to wound problems. Nonunion was developed in the medial malleolus in 4 patients. Revision surgery was performed because of implant irritation in 2 patients and early fixation loss in the medial malleolus fracture in one patient. Calcaneotibial arthrodesis was performed in 3 patients because of implant failure and ankle luxation associated with non-union. A correlation was determined between ASA score and DM and complications, but not with osteoporosis. The mean follow-up AOFAS score was 86.7 ± 12.5 (range, 36-100).A total of 94 (84.7%) patients could walk without assistance postoperatively and 92 (82.9%) were able to regain the preoperative level of mobilization. Conclusion: Although surgery can be considered an appropriate treatment option for ankle fractures in patients aged >65 years, care must be taken to prevent potential complications and the necessary precautions must be taken against correctable comorbidities.

scholarly journals Importance of a Follow-Up Ultrasound Protocol in Monitoring Posttraumatic Spleen Complications in Children Treated with a Non-Operative Management

Medicina ◽  
2021 ◽  
Vol 57 (8) ◽  
pp. 734
Author(s):  
Ivona Djordjevic ◽  
Dragoljub Zivanovic ◽  
Ivana Budic ◽  
Ana Kostic ◽  
Danijela Djeric
Keyword(s):  
Splenic Abscess ◽  
Operative Management ◽  
High Energy ◽  
Significant Difference ◽  
Injury Grade ◽  
Grade Ii ◽  
The Mean ◽  
Non Operative Management ◽  
Grade Iii

Background and objectives: For the last three decades, non-operative management (NOM) has been the standard in the treatment of clinically stable patients with blunt spleen injury, with a success rate of up to 95%. However, there are no prospective issues in the literature dealing with the incidence and type of splenic complications after NOM. Materials and methods: This study analyzed 76 pediatric patients, up to the age of 18, with blunt splenic injury who were treated non-operatively. All patients were included in a posttraumatic follow-up protocol with ultrasound examinations 4 and 12 weeks after injury. Results: The mean age of the children was 9.58 ± 3.97 years (range 1.98 to 17.75 years), with no statistically significant difference between the genders. The severity of the injury was determined according to the American Association for Surgery of Trauma (AAST) classification: 7 patients had grade I injuries (89.21%), 21 patients had grade II injuries (27.63%), 33 patients had grade III injuries (43.42%), and 15 patients had grade IV injuries (19.73%). The majority of the injuries were so-called high-energy ones, which were recorded in 45 patients (59.21%). According to a previously created posttraumatic follow-up protocol, complications were detected in 16 patients (21.05%). Hematomas had the highest incidence and were detected in 11 patients (14.47%), while pseudocysts were detected in 3 (3.94%), and a splenic abscess and pseudoaneurysm were detected in 1 patient (1.31%), respectively. The complications were in a direct correlation with injury grade: seven occurred in patients with grade IV injuries (9.21%), five occurred in children with grade III injuries (6.57%), three occurred in patients with grade II injuries (3.94%), and one occurred in a patient with a grade I injury (1.31%). Conclusion: Based on the severity of the spleen injury, it is difficult to predict the further course of developing complications, but complications are more common in high-grade injuries. The implementation of a follow-up ultrasound protocol is mandatory in all patients with NOM of spleen injuries for the early detection of potentially dangerous and fatal complications.

scholarly journals Development of Spanish Broom and Flax Dressings with Glycyrrhetinic Acid-Loaded Films for Wound Healing: Characterization and Evaluation of Biological Properties

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1192
Author(s):  
Angela Abruzzo ◽  
Concettina Cappadone ◽  
Valentina Sallustio ◽  
Giovanna Picone ◽  
Martina Rossi ◽  
...  
Keyword(s):  
Wound Healing ◽  
Drug Loading ◽  
Healing Process ◽  
In Vitro Release ◽  
Sodium Hyaluronate ◽  
Biological Properties ◽  
Glycyrrhetinic Acid ◽  
Wound Dressings ◽  
Biological Studies

The selection of an appropriate dressing for each type of wound is a very important procedure for a faster and more accurate healing process. So, the aim of this study was to develop innovative Spanish Broom and flax wound dressings, as alternatives to cotton used as control, with polymeric films containing glycyrrhetinic acid (GA) to promote wound-exudate absorption and the healing process. The different wound dressings were prepared by a solvent casting method, and characterized in terms of drug loading, water uptake, and in vitro release. Moreover, biological studies were performed to evaluate their biocompatibility and wound-healing efficacy. Comparing the developed wound dressings, Spanish Broom dressings with GA-loaded sodium hyaluronate film had the best functional properties, in terms of hydration ability and GA release. Moreover, they showed a good biocompatibility, determining a moderate induction of cell proliferation and no cytotoxicity. In addition, the wound-healing test revealed that the Spanish Broom dressings promoted cell migration, further facilitating the closure of the wound.

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