Lightening Effect of Skin Lightening Cream Containing Piper betle L. Extract in Human Volunteers

Hyperpigmentation affects people globally with negative psychological impacts. Piper betle L. leaf (PBL) extract has many benefits including skin lightening which may reduce hyperpigmentation. The objective of this study was to develop an effective skin-lightening cream containing PBL with ideal characteristics. A formulation of base cream and PBL cream was prepared and characterized by centrifugation, particle size and zeta potential analysis, rheological profile studies and physical properties’ observation. In vivo studies on 30 human subjects tested the effects of base and PBL cream on skin-lightening, hydration, trans-epidermal water loss (TEWL) and elasticity through weekly tests 4 weeks in duration. Base and PBL creams had a non-Newtonian property with acceptable color, odor, texture, zeta potential, particle size and showed no phase separation. The in vivo study indicated a significant reduction in melanin content and an improvement in skin tone for PBL cream but not in base cream. TEWL and elasticity also showed significant reduction for both formulations, indicating a healthier skin barrier and supple skin with consistent use, although hydration fluctuated with no significant changes. The developed PBL cream showed significant results in the reduction in melanin content and improving skin tone, which shows the formulation can confer skin-lightening effect.

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in vitro- and in vivo Evaluation of Methotrexate-Loaded Hydrogel Nanoparticles Intended to Treat Primary CNS Lymphoma via Intranasal Administration

Journal of Pharmacy & Pharmaceutical Sciences ◽

10.18433/jpps29496 ◽

2018 ◽

Vol 21 ◽

pp. 305-317 ◽

Cited By ~ 6

Author(s):

Leila Pourtalebi Jahromi ◽

Soliman Mohammadi-Samani ◽

Reza Heidari ◽

Amir Azadi

Keyword(s):

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

Intranasal Administration ◽

Free Drug ◽

In Vivo Studies ◽

Nano Formulation ◽

The Brain ◽

Drug Solution

Purpose: Although it passes through blood-brain barrier (BBB) very poorly, methotrexate (MTX) is an important therapeutic in the treatment of many central nervous system malignancies. Accordingly, intranasal (IN) administration accompanied with a muco-adhesive chitosan-based nanoformulation is expected to overcome this problem. Methods: Nanogel containing MTX was prepared through an ionic gelation method and then characterized in terms of particle size, morphology, zeta potential, drug loading and drug release behavior. The drug release results were fitted on eight mathematical models to choose the model best describing the phenomenon. Then the nano-formulation and free drug solution in deionized water as control were administered in the nasal cavity for rats and after 15, 30, 60 and 240 minutes their brain and plasma were analyzed for MTX quantity. Results: The nano-formulation demonstrated an average particle size near 100 nm with a zeta potential of 18.65±1.77 mv. Loading efficiency and loading capacity were calculated to be 65.46±7.66 and 3.02±0.34 respectively. The Weibull model was found to be best describing the release phenomenon as a combination of swelling and Fickian diffusion. Moreover in in vivo studies, drug targeting efficiency and direct transport percentage for nanogel (test) and free drug solution (control) were 424.88% and 76.46% and 34842.15% and 99.71% respectively. Conclusion: According to in vivo studies, nanogel produced significantly higher concentration of MTX in the brain but not in the plasma when compared to the free drug solution. Besides, in comparison to intravenous administration of the same nanogel it was indicated that intranasal administration significantly increases the brain concentration of MTX.

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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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Preparation and preclinical evaluation of aceclofenac loaded pectinate mucoadhesive microspheres

Drugs and Therapy Studies ◽

10.4081/dts.2012.e8 ◽

2012 ◽

Vol 2 (1) ◽

pp. 8 ◽

Cited By ~ 1

Author(s):

Santanu Chakraborty ◽

Priyanka Nayak ◽

Bala Murali Krishna ◽

Madhusmruti Khandai ◽

Ashoke Kumar Ghosh

Keyword(s):

Particle Size ◽

Drug Release ◽

Polymer Concentration ◽

Research Work ◽

In Vivo Studies ◽

Systemic Absorption ◽

Cross Linking ◽

Significant Difference

The aim of the present research work was to fabricate aceclofenac loaded pectinate microspheres by ionic gelation method and evaluate the effect of different cross-linking agents and polymer concentration on particle size, encapsulation efficacy and drug release behavior. It was also investigated that whether this pectinate dosage form was able to target the drug release in intestinal region and prevent the different side effect associated with the drug in stomach or not. It was observed that particle size, encapsulation efficacy and in vitro drug release were largely depended on polymer concentration and cross-linking agents. It was also observed that pectinate microspheres showed excellent pH depended mucoadhesive properties and they were able to restrict the drug release in stomach. In vitro drug release study showed that alminium-pectinate microspheres have more sustaining property as compared to barium-pectinate microspheres. Holm-Sidak multiple comparison analysis suggested a significant difference in measured t50% values among all the formulations with same cross-linking agent. In vivo studies revealed that the anti inflammatory and analgesic effects induced by pectinate microspheres were significantly high and prolonged as compared to pure drug. So, pectinate microspheres can be an excellent carrier for targeting the delivery of aceclofenac as well as help in improving the patient compliance by prolonging the systemic absorption.

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Formulation and Characterization of Carvedilol Leciplex for Glaucoma Treatment: In-Vitro, Ex-Vivo and In-Vivo Study

Pharmaceutics ◽

10.3390/pharmaceutics10040197 ◽

2018 ◽

Vol 10 (4) ◽

pp. 197 ◽

Cited By ~ 9

Author(s):

Doaa Hassan ◽

Rehab Abdelmonem ◽

Menna Abdellatif

Keyword(s):

Particle Size ◽

Intraocular Pressure ◽

Zeta Potential ◽

Ex Vivo ◽

Entrapment Efficiency ◽

Molar Ratio ◽

Duration Of Action ◽

Corneal Permeability ◽

Glaucoma Treatment

This study evaluated the efficacy of cationic nanoparticle (leciplex) to deliver carvedilol to ocular surface for glaucoma treatment as recent studies pointed out the effect of topical carvedilol on intraocular pressure, therefore carvedilol loaded leciplex formulae were prepared using soy phosphatidyl choline (SPC) and cationic surfactant (CTAB/DDAB) and characterized for morphology, entrapment efficiency, particle size, zeta potential and ex-vivo corneal permeation. Then the selected formula was evaluated via in-vivo studies in comparison with carvedilol solution. Leciplex nanoparticles appeared spherical in shape with entrapment efficiency exceeded 95% in all formulae. Leciplex formula composed of SPC and DDAB in (1:1) molar ratio showed the smallest particle size (16.04 ± 1.2 nm), highest zeta potential value (53.9 ± 0.91 mv) and highest apparent corneal permeability coefficient (0.1157 cm/h). Carvedilol leciplex reduced intraocular pressure (IOP) to normal range in ocular hypertensive rabbits after 30 min and duration of action lasted for 24 h, while carvedilol solution reduced IOP to normal value after 60 min and duration of action lasted for 6 h. Furthermore, histological examination of eyeballs of rabbits treated with carvedilol leciplex showed improvement of retinal atrophy of glaucomatous eyes. This study concluded that leciplex improve transcorneal permeation and bioavailability of carvedilol.

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Atorvastatin calcium loaded chitosan nanoparticles: in vitro evaluation and in vivo pharmacokinetic studies in rabbits

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502015000200024 ◽

2015 ◽

Vol 51 (2) ◽

pp. 467-477 ◽

Cited By ~ 13

Author(s):

Abdul Baquee Ahmed ◽

Ranjit Konwar ◽

Rupa Sengupta

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Oral Bioavailability ◽

Chitosan Nanoparticles ◽

Rabbit Model ◽

Pharmacokinetic Studies ◽

Release Formulation ◽

Atorvastatin Calcium

In this study, we prepared atorvastatin calcium (AVST) loaded chitosan nanoparticles to improve the oral bioavailability of the drug. Nanoparticles were prepared by solvent evaporation technique and evaluated for its particle size, entrapment efficiency, zeta potential, <italic>in vitro</italic> release and surface morphology by scanning electron microscopy (SEM). In addition, the pharmacokinetics of AVST from the optimized formulation (FT5) was compared with marketed immediate release formulation (Atorva(r)) in rabbits. Particle size of prepared nanoparticles was ranged between 179.3 ± 7.12 to 256.8 ± 8.24 nm with a low polydispersity index (PI) value. Zeta potential study showed that the particles are stable with positive values between 13.03 ± 0.32 to 46.90 ± 0.49 mV. FT-IR studies confirmed the absence of incompatibility of AVST with excipient used in the formulations. <italic>In vitro</italic> release study showed that the drug release was sustained for 48 h. Results of pharmacokinetics study showed significant changes in the pharmacokinetic parameter (2.2 fold increase in AUC) of the optimized formulation as compared to marketed formulation (Atorva(r)). Thus, the developed nanoparticles evidenced the improvement of oral bioavailability of AVST in rabbit model.

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Enhanced Oral Bioavailability of Celecoxib Nanocrystalline Solid Dispersion based on Wet Media Milling Technique: Formulation, Optimization and In Vitro/In Vivo Evaluation

Pharmaceutics ◽

10.3390/pharmaceutics11070328 ◽

2019 ◽

Vol 11 (7) ◽

pp. 328 ◽

Cited By ~ 9

Author(s):

Zhuang Ding ◽

Lili Wang ◽

Yangyang Xing ◽

Yanna Zhao ◽

Zhengping Wang ◽

...

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Solid Dispersion ◽

Oral Bioavailability ◽

Stability Study ◽

Sprague Dawley ◽

Scanning Calorimetry ◽

In Vivo Evaluation

Celecoxib (CLX), a selective COX-2 inhibitor, is a biopharmaceutics classification system (BCS) class II drug with its bioavailability being limited by thepoor aqueoussolubility. The purpose of this study was to develop and optimize CLX nanocrystalline(CLX-NC) solid dispersion prepared by the wet medium millingtechnique combined with lyophilizationto enhance oral bioavailability. In formulation screening, the resulting CLX-NC usingpolyvinylpyrrolidone (PVP) VA64 and sodiumdodecyl sulfate (SDS) as combined stabilizers showed the minimum particle size and a satisfactory stability. The formulation and preparation processwere further optimized by central composite experimentaldesign with PVP VA64 concentration (X1), SDS concentration (X2) and milling times (X3) as independent factors and particle size (Y1), polydispersity index (PDI, Y2) and zeta potential (Y3) as response variables. The optimal condition was determined as a combination of 0.75% PVP VA64, 0.11% SDS with milling for 90 min.The particle size, PDI and zeta potential of optimized CLX-NC were found to be 152.4 ± 1.4 nm, 0.191 ± 0.012 and −34.4 ± 0.6 mV, respectively. The optimized formulation showed homogeneous rod-like morphology as observed by scanning electron microscopy and was in a crystalline state as determined by differential scanning calorimetry and powder X-ray diffraction. In a storage stability study, optimized CLX-NC exhibited an excellent physical stability during six months’ storage at both the refrigeration and room conditions. In vivo pharmacokinetic research in Sprague-Dawley ratsdisplayed that Cmax and AUC0–∞ of CLX-NC were increased by 2.9 and 3.1 fold, compared with physical mixture. In this study, the screening and optimizing strategy of CLX-NC formulation represents a commercially viable approach forenhancing the oral bioavailability of CLX.

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A Novel Sustained Anti-Inflammatory Effect of Atorvastatin—Calcium PLGA Nanoparticles: In Vitro Optimization and In Vivo Evaluation

Pharmaceutics ◽

10.3390/pharmaceutics13101658 ◽

2021 ◽

Vol 13 (10) ◽

pp. 1658

Author(s):

Dalia H. Abdelkader ◽

Ahmed Kh. Abosalha ◽

Mohamed A. Khattab ◽

Basmah N. Aldosari ◽

Alanood S. Almurshedi

Keyword(s):

Particle Size ◽

Zeta Potential ◽

In Vitro Release ◽

In Vivo Evaluation ◽

Water Emulsion ◽

Atorvastatin Calcium ◽

Anti Inflammatory ◽

Inflammatory Effect

Atorvastatin Calcium (At-Ca) has pleiotropic effect as anti-inflammatory drug beside its main antihyperlipidemic action. Our study was conducted to modulate the anti-inflammatory effect of At-Ca to be efficiently sustained for longer time. Single oil-water emulsion solvent evaporation technique was used to fabricate At-Ca into polymeric nanoparticles (NPs). In vitro optimization survey was performed on Poly(lactide-co-glycolide) (PLGA) loaded with At-Ca regrading to particle size, polydispersity index (PDI), zeta potential, percent entrapment efficiency (% EE), surface morphology and in vitro release pattern. In vitro drug-polymers interactions were fully scanned using Fourier-Transform Infrared Spectroscopy (FTIR) and Differential Scanning calorimetry (DSC) proving that the method of fabrication is an optimal strategy maintaining the drug structure with no interaction with polymeric matrix. The optimized formula with particle size (248.2 ± 15.13 nm), PDI (0.126 ± 0.048), zeta potential (−12.41 ± 4.80 mV), % EE (87.63 ± 3.21%), initial burst (39.78 ± 6.74%) and percent cumulative release (83.63 ± 3.71%) was orally administered in Male Sprague–Dawley rats to study the sustained anti-inflammatory effect of At-Ca PLGA NPs after carrageenan induced inflammation. In vivo results demonstrate that AT-Ca NPs has a sustained effect extending for approximately three days. Additionally, the histological examination revealed that the epidermal/dermal layers restore their typical normal cellular alignment with healthy architecture.

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Preparation and Characterization of Betel Leaves (Piper betle Linn) Extract Nanoparticle with Ionic Gelation Method

Journal Of Tropical Pharmacy And Chemistry ◽

10.25026/jtpc.v5i1.224 ◽

2020 ◽

Vol 5 (1) ◽

Author(s):

Dwi Saryanti ◽

Dian Nugraheni ◽

Nisa Sindi Astuti

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Leaf Extract ◽

Particle Morphology ◽

Particle Size Analysis ◽

Size Analysis ◽

Piper Betle ◽

Ionic Gelation ◽

Betel Leaf

Nanoparticles are used in drug delivery which can increase mass transfer so increase the absorption and effectiveness of the drug. Therefore, its prospect to improve antibacterial and antioxidants activities of betel leaves. The research aimed to preparation and characterization of betel leaf extract using ionic gelation technique. The formulation of nanoparticles from betel leaf extract with ionic gelation method using alginate and CaCl2 with a ratio of 2.5: 1. The characterization of the nanoparticles includes particle size analysis, zeta potential, particle morphology and determination of flavonoid content. Particle size analysis demonstrated that the betel leaf extract nanoparticles had a particle size of 243,03 ± 1,48 nm, zeta potential of -23,0 ± 0,35 mV and morphology of particle showed that a flat shape. The betle leaf exctract nanoparticle positively contained flavonoid with Rf 0.7 equivalent to quercetin. The betel leaf extract can be made nanoparticles with ionic gelation method using alginate and CaCl2.

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Nobiletin-loaded composite penetration enhancer vesicles restore the normal miRNA expression and the chief defence antioxidant levels in skin cancer

Scientific Reports ◽

10.1038/s41598-021-99756-1 ◽

2021 ◽

Vol 11 (1) ◽

Author(s):

Mahitab Bayoumi ◽

Mona G. Arafa ◽

Maha Nasr ◽

Omaima A. Sammour

Keyword(s):

Particle Size ◽

Skin Cancer ◽

Zeta Potential ◽

Ex Vivo ◽

Physical Stability ◽

Entrapment Efficiency ◽

Penetration Enhancer ◽

Oxidative Stress Biomarkers ◽

Skin Deposition

AbstractSkin cancer is one of the most dangerous diseases, leading to massive losses and high death rates worldwide. Topical delivery of nutraceuticals is considered a suitable approach for efficient and safe treatment of skin cancer. Nobiletin; a flavone occurring in citrus fruits has been reported to inhibit proliferation of carcinogenesis since 1990s, is a promising candidate in this regard. Nobiletin was loaded in various vesicular systems to improve its cytotoxicity against skin cancer. Vesicles were prepared using the thin film hydration method, and characterized for particle size, zeta potential, entrapment efficiency, TEM, ex-vivo skin deposition and physical stability. Nobiletin-loaded composite penetration enhancer vesicles (PEVs) and composite transfersomes exhibited particle size 126.70 ± 11.80 nm, 110.10 ± 0.90 nm, zeta potential + 6.10 ± 0.40 mV, + 9.80 ± 2.60 mV, entrapment efficiency 93.50% ± 3.60, 95.60% ± 1.50 and total skin deposition 95.30% ± 3.40, 100.00% ± 2.80, respectively. These formulations were selected for cytotoxicity study on epidermoid carcinoma cell line (A431). Nobiletin-loaded composite PEVs displayed the lowest IC50 value, thus was selected for the in vivo study, where it restored skin condition in DMBA induced skin carcinogenesis mice, as delineated by histological and immuno-histochemical analysis, biochemical assessment of skin oxidative stress biomarkers, in addition to miRNA21 and miRNA29A. The outcomes confirmed that nobiletin- loaded composite PEVs is an efficient delivery system combating skin cancer.

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Hering-Breuer Reflex and pre-Botzinger Complex: A Literature Survey

Journal of Bangladesh Society of Physiologist ◽

10.3329/jbsp.v2i0.988 ◽

1970 ◽

Vol 2 ◽

pp. 89-94

Author(s):

M Ahmed

Keyword(s):

Human Subjects ◽

Respiratory Rhythm ◽

Physiological Role ◽

Personal Communication ◽

In Vivo Studies ◽

Respiratory Rhythmogenesis ◽

Neuronal Regulation ◽

Bötzinger Complex

The existence and physiological role of Hering-Breuer reflex and pre-Botzinger complex has long been depreciated by the Bangladesh society of physiologist (personal communication). The aim of this mini review is to highlight the recent findings on the aforementioned topics. Due to the difficulties in vivo studies in human subjects, many aspects of the neuronal regulation of the respiratory rhythm are still unclear. However, the recent localization of the pre-Botzinger complex in humans and advances in technologies necessitates further exploration of the neuronal circuits in the pre-BotC complex which will subsequently unwrap the magical box and pave the way to solve the puzzle of the mechanism of respiratory rhythmogenesis and its modulation in different pathophysiological conditions. Key Words: Physiology; Hering-Breuer reflex; pre-Botzinger complex; Rhythmic respiration DOI:10.3329/jbsp.v2i0.988 J Bangladesh Soc Physiol. 2007 Dec;(2):89-94.

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