In Vitro Estimation of Photo-Protective Potential of Pomegranate Seed Oil and Development of a Nanoformulation

Background: Since ancient times, people have been using natural resources for photoprotection purposes. One such highly recognised natural agent is pomegranate seed oil, considered as wonder oil owing to the presence of several beneficial phytoconstituents. Objective: The study aimed to establish the photoprotective potential of pomegranate seed oil through various in vitro and biochemical studies along with the formation of nanoemulsion, an efficient topical delivery system for the oil. Method: Photo-protective potential of the oil was estimated by determining in vitro antioxidant and anti-inflammatory activity, total phenolic content, anti elastase, antihyaluronidase and anticollagenase activities of the oil. Ultrasonication method was used to formulate nanoemulsions. The optimisation was done following the central composite design. The characterisation was done by particle size analysis, zeta potential, polydispersity index, pH, viscosity, stability testing and transmission electron microscopy. The optimised nanoemulsion was loaded into a gel base for topical application and further release studies were carried out. Results: The IC50 values of anti-elastase, anti-collagenase and anti-hyaluronidase were found to be 309 mg/ml, 4 mg/ml and 95 mg/ml respectively. The results of anti-oxidant and anti-inflammatory activity were also significant, which thereby established the photo-protective potential of the oil. The optimum batch 2 had particle size 83.90 nm, 0.237 PDI and -5.37 mV zeta potential. The morphology was confirmed by TEM. Batch 2 was incorporated into a gel base and release studies showed 74.12 % release within 7 hours. Conclusion: Pomegranate seed oil possesses a potential photo-protective ability. Nanoemulsions proved to be a promising carrier for the topical delivery of the oil.

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Pomegranate Seed Oil Modulates Functions and Survival of BV-2 Microglial Cells in vitro

International Journal for Vitamin and Nutrition Research ◽

10.1024/0300-9831/a000216 ◽

2014 ◽

Vol 84 (5-6) ◽

pp. 295-309 ◽

Cited By ~ 5

Author(s):

Lucia Račková ◽

Volkan Ergin ◽

Elif Burcu Bali ◽

Marcela Kuniaková ◽

Çimen Karasu

Keyword(s):

Seed Oil ◽

Therapeutic Potential ◽

Fold Increase ◽

Punica Granatum ◽

Current Evidence ◽

No Production ◽

Omega 3 ◽

Pomegranate Seed Oil ◽

Pomegranate Seed

Abstract. Current evidence has demonstrated the immunomodulatory efficacy of omega-3 polyunsaturated fatty acids (PUFAs) in glial cells, suggesting their therapeutic potential for diseases in the central nervous system (CNS). However, conjugated omega-5 PUFAs have also attracted considerable attention because of their suggested anti-inflammatory effects. In the present study, the effect of pomegranate (Punica granatum L.) seed oil (PSEO) (a rich source of omega-5 PUFAs) on the activation of cultured BV-2 microglia was investigated within a 24-hour incubation period. PSEO (25 μg/ml) showed only a slightly smaller inhibitory effect on LPS-stimulated NO production (243 ± 12.5 % of control, p<0.001 vs. 437 ± 9.2 % in stimulated cells) and TNF-α release (87.1 ± 5.62 pg/ml vs. 229 ± 24.4 pg/ml in stimulated cells), as well as iNOS expression (7.36-fold of control, p < 0.01, vs. 17.5-fold increase in stimulated cells) compared to a standardized omega-3 PUFAs mixture (25 μg/ml) and the flavonoid quercetin (25 μmol/l). Unlike quercetin and stobadine, only the PUFA preparations effectively prevented apoptosis of microglia (as confirmed by the suppression of caspase 3 activation) exposed to the toxic concentration of LPS. The PUFA preparations did not provide a notable suppression of the intracellular oxidant generation and did not influence the intracellular distribution of cholesterol (as confirmed by filipin staining). However, they appeared to affect the morphology of activated cells. In conclusion, our data point to the first evidence of immunomodulation and cytoprotection of BV-2 microglia by the pomegranate seed oil, indicating that it may be (comparably to omega-3 PUFAs) efficient against microglia-mediated neuroinflammation while preventing the premature depletion of these immune effector cells in the brain.

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Role of Hypericum perforatum oil and pomegranate seed oil in wound healing: an in vitro study

Zeitschrift für Naturforschung C ◽

10.1515/znc-2020-0301 ◽

2021 ◽

Vol 0 (0) ◽

Author(s):

Ebru Uzunhisarcıklı ◽

Mükerrem Betül Yerer

Keyword(s):

Wound Healing ◽

Hypericum Perforatum ◽

Seed Oil ◽

In Vitro Study ◽

Seed Extract ◽

Hacat Cells ◽

Pomegranate Seed Oil ◽

Pomegranate Seed ◽

Better Than

Abstract This study aimed to investigate the wound-healing efficacy of Hypericum perforatum and pomegranate seed extract oil combined with curcumin as an anti inflammatory agent. A series of experiments were carried out to determine effective concentrations for H. perforatum oil, pomegranate seed extract oil, and curcumin. Ibuprofen was used as a positive control. The wound-healing effects of the applied compounds were tested according to the migration experiment model performed in HaCaT cells. A real-time cell analyzer (xCELLigence) was used to determine the cytotoxic/proliferative effects of H. perforatum, pomegranate seed oil, ibuprofen, and curcumin in HaCaT cells alone and their combined use at specified concentrations. After examining the noncytotoxic concentrations of H. perforatum oil, pomegranate seed oil, curcumin, and ibuprofen, migration experiments were performed to examine the wound healing properties. According to the results, the wound-healing efficacy of curcumin and H. perforatum combination was better than ibuprofen combinations. Also, according to the results, the wound-healing efficacy of curcumin and pomegranate seed oil combination was better than ibuprofen combinations. It was concluded that both oils had improved wound-healing properties in combination with curcumin or Ibuprofen.

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Valsartan Loaded Solid Lipid Nanoparticles: Development, Characterization, and In vitro and Ex vivo Evaluation

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2011.4.3.7 ◽

2011 ◽

Vol 4 (3) ◽

pp. 1483-1490

Author(s):

Krutika K Sawant ◽

B Parmar ◽

S A Mandal ◽

K C Petkar ◽

L D Patel

Keyword(s):

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

Solid Lipid Nanoparticles ◽

Ex Vivo ◽

Hepatic Metabolism ◽

Lipid Nanoparticles ◽

Release Studies ◽

First Pass

Valsartan is an antihypertensive drug with poor oral bioavailability ranging from 10-35% because of poor solubility, dissolution and most importantly, extensive first pass hepatic metabolism. The present study deals with the development and characterization of Valsartan-loaded solid lipid nanoparticles (VSLNs) to enhance the solubility, bypass the first pass hepatic metabolism, and enhance the lymphatic absorption leading to improved bioavailability. VSLNs were developed using glyceryl behenate (Compritol 888 ATO®) as the lipid and Poloxamer 407 (Pluronic F 127) as the surfactant by the solvent injection method. VSLNs were characterized for mean particle Size (MPS), zeta potential, percentage drug entrapment (PDE), DSC Scans, XRD and TEM analysis. In vitro drug release studies were performed in 0.067 M phosphate buffer of pH 6.8 using dialysis diffusion bag method. Ex vivo drug release studies were also performed for both VSLNs and valsartan suspension in stomach and intestine. The optimized formulation of having the 80 mg lipid, 10 mg drug and 250 mg surfactant was found to have particle size distribution of 142.5 ± 1.859 nm, zeta potential of – 14.3 ± 0.384 mV, and 84.59 ± 0.328% drug entrapment. Based on these results, it is concluded that SLNs show promise for improving the oral bioavailability of valsartan.

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SELF-ASSEMBLED CHITOSAN NANOPARTICLES FOR PERCUTANEOUS DELIVERY OF CAFFEINE: PREPARATION, CHARACTERIZATION AND IN VITRO RELEASE STUDIES

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i4.25947 ◽

2018 ◽

Vol 10 (4) ◽

pp. 172 ◽

Cited By ~ 1

Author(s):

Nik Amanina Farhanah Abu Hassan ◽

Shariza Sahudin ◽

Zahid Hussain ◽

Mumtaz Hussain ◽

Mumtaz Hussain

Keyword(s):

Electron Microscopy ◽

Particle Size ◽

Zeta Potential ◽

Surface Charge ◽

Process Parameters ◽

In Vitro Release ◽

Freeze Dried ◽

Release Studies ◽

Vitro Release

Objective: Chitosan (CS)–tripolyphosphate (TPP)–nanoparticles (NPs) have been extensively studied during the past few decades due to their well-recognized applicability in various fields. The present study attempts to optimise the development of these nanoparticles to enhance the percutaneous delivery of caffeine.Methods: CS-TPP-NPs were prepared via ionic cross-linking of CS and TPP and were characterized. The influence of several formulation conditions (CS: TPP mass ratio and concentration of caffeine) and process parameters (stirring speed, stirring time and ultra-sonication time) on the colloidal characteristics of CS-TPP-NPs were investigated and the resulting nanoparticles were characterized using scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared (FTIR) and x-ray diffraction (XRD) analyses. Physicochemical properties, including particle size, zeta potential and polydispersity index (PDI) were examined, and in vitro release studies were conducted to ascertain the release profile of caffeine from the nanoparticles. In addition, the colloidal stability of the prepared NPs was also assessed on storage.Results: Process parameters appeared to exert a significant effect on the physicochemical characteristics of the CS-TPP-NPs. The CS-TPP-NPs prepared under optimum conditions (CS concentration of 0.2 mg/ml, CS: TPP volume ratio of 25:12 ml, stirred at 700 rpm for 60 min, with 0.97 mg/ml caffeine concentration and treatment with low ultra-sonication for 30 min) had shown a mean particle size of ~143.43±1.69 nm, zeta potential of+43.13±1.10 mV, PDI of ~0.30±0.01. A drug loading capacity and encapsulation efficiency of 48.89% and 60.69%, respectively, were obtained. Cumulative release study for drug-loaded CS-NPs was significantly (p<0.001, paired t-test) higher (58.7% caffeine released) compared to control formulation (41.5% caffeine released) after 72 h. Stability studies conducted for 28 d showed that caffeine-loaded CS-NPs degraded much quicker when stored at 25 ⁰C than 4 ⁰C. It was also noted that caffeine-loaded CS-NPs in the freeze-dried form were unstable as the surface charge of nanoparticles dropped from positive zeta potential to-3.55 mV within 2 d at 4 ⁰C and at 25 ⁰C, surface charge dropped to-3.16 mV within 14 d of the experiment.Conclusion: Chitosan (CS)–tripolyphosphate (TPP)–nanoparticles (NPs) appear to be a promising strategy to achieve sustained percutaneous delivery of caffeine.

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Formulation and Evaluation of Nanosuspension of Simvastatin

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2015.8.2.9 ◽

2015 ◽

Vol 8 (2) ◽

pp. 2858-2873

Author(s):

Rupali L. Shid ◽

Shashikant N. Dhole ◽

Nilesh Kulkarni ◽

Santosh L Shid

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Factorial Design ◽

Dissolution Rate ◽

In Vitro Dissolution ◽

Total Drug ◽

23 Factorial Design ◽

Rate Of Dissolution

Poor water solubility and slow dissolution rate are issues for the majority of upcoming and existing biologically active compounds. Simvastatin is poorly water-soluble drug and its bioavailability is very low from its crystalline form. The purpose of this study wasto increase the solubility and dissolution rate of simvastatin by the preparation of nanosuspension by emulsification solvent diffusion method at laboratory scale. Prepared nanosus-pension was evaluated for its particle size and in vitro dissolution study and characterized by zeta potential,differential scanning calorimetry (DSC) and X-Ray diffractometry (XRD), motic digital microscopy, entrapment efficiency, total drug content, saturated solubility study and in vivo study. A 23 factorial design was employed to study the effect of independent variables, amount of SLS (X1), amount of PVPK-30 (X2) and poloxamer-188 (X3) and dependent variables are total drug content and polydispersity Index. The obtained results showed that particle size (nm) and rate of dissolution has been improved when nanosuspension prepared with the higherconcentration of PVPK-30 with the higher concentration of PVP K-30 and Poloxamer-188 and lower concentration of SLS. The particle size and zeta potential of optimized formulation was found to be 258.3 nm and 23.43. The rate of dissolution of the optimized nanosuspension was enhanced (90% in 60min), relative to plain simvastatin (21% in 60 min), mainly due to the formation of nanosized particles. These results indicate the suitability of 23 factorial design for preparation of simvastatin loaded nano-suspension significantly improved in vitro dissolution rate and thus possibly enhance fast onset of therapeutic drug effect. In vivo study shows increase in bioavailability in nanosuspension formulation than the plain simvastatin drug.

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Optimization and Characterization of Aqueous Micellar Formulations for Ocular Delivery of an Antifungal Drug, Posaconazole

Current Pharmaceutical Design ◽

10.2174/1381612826666200313172207 ◽

2020 ◽

Vol 26 (14) ◽

pp. 1543-1555 ◽

Cited By ~ 2

Author(s):

Meltem E. Durgun ◽

Emine Kahraman ◽

Sevgi Güngör ◽

Yıldız Özsoy

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Size Distribution ◽

Encapsulation Efficiency ◽

Fungal Infections ◽

In Vitro Release ◽

Pluronic F127 ◽

Glycol Succinate ◽

Vitro Release

Background: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. Objective: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. Method: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. Results: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. Conclusion: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.

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Moxifloxacin Hydrochloride-Loaded Eudragit® RL 100 and Kollidon® SR Based Nanoparticles: Formulation, In vitro Characterization and Cytotoxicity.

Combinatorial Chemistry & High Throughput Screening ◽

10.2174/1386207323666200428091945 ◽

2020 ◽

Vol 23 ◽

Cited By ~ 2

Author(s):

Gülsel Yurtdaş Kırımlıoğlu ◽

Sinan Özer ◽

Gülay Büyükköroğlu ◽

Yasemin Yazan

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Spray Drying ◽

Prolonged Release ◽

Ocular Delivery ◽

Corneal Permeability ◽

Release Pattern ◽

In Vitro Characterization ◽

Ocular Bioavailability

Background: Considering the low ocular bioavailability of conventional formulations used for ocular bacterial infection treatment, there’s a need for designing efficient novel drug delivery systems that may enhance of precorneal retention time and corneal permeability. Aim and Objective: The current research focuses on developing nanosized and non-toxic Eudragit® RL 100 and Kollidon® SR nanoparticles loaded with moxifloxacin hydrochloride (MOX) for its prolonged release to be promising for effective ocular delivery. Methods: In this study, MOX was incorporation was carried out by spray drying method aiming ocular delivery. In vitro characteristics were evaluated in detail with different methods. Results: MOX was successfully incorporated into Eudragit® RL 100 and Kollidon® SR polymeric nanoparticles by spray-drying process. Particle size, zeta potential, entrapment efficiency, particle morphology, thermal, FTIR, XRD and NMR analyses and MOX quantification using HPLC method were carried out to evaluate the nanoparticles prepared. MOX loaded nanoparticles demonstrated nanosized and spherical shape while in vitro release studies demonstrated modified release pattern which followed Korsmeyer-Peppas kinetic model. Following successful incorporation of MOX into the nanoparticles, the formulation (MOX: Eudragit® RL 100, 1:5) (ERL-MOX 2) was selected for further studies by the reason of its better characteristics like cationic zeta potential, smaller particle size, narrow size distribution and more uniform prolonged release pattern. Moreover, ERL-MOX 2 formulation remained stable for 3 months and demonstrated higher cell viability values for MOX. Conclusion: In vitro characterization analyses showed that non-toxic, nano-sized and cationic ERLMOX 2 formulation has the potential of enhancing ocular bioavailability.

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