scholarly journals Development of a Topical Amphotericin B and Bursera graveolens Essential Oil-Loaded Gel for the Treatment of Dermal Candidiasis

2021 ◽  
Vol 14 (10) ◽  
pp. 1033
Author(s):  
Lupe Carolina Espinoza ◽  
Lilian Sosa ◽  
Paulo C. Granda ◽  
Nuria Bozal ◽  
Natalia Díaz-Garrido ◽  
...  
Keyword(s):  
Essential Oil ◽  
Amphotericin B ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Topical Administration ◽  
In Vivo Models ◽  
Topical Gel ◽  
Cutaneous Candidiasis ◽  
Vitro Release

The higher molecular weight and low solubility of amphotericin B (AmB) hinders its topical administration. The aim of this study was to incorporate Bursera graveolens essential oil into an AmB topical gel (AmB + BGEO gel) in order to promote the diffusion of the drug through the skin in the treatment of cutaneous candidiasis. AmB + BGEO gel formulation was determined using a factorial experiment. Physical and chemical parameters, stability, in vitro release profile and ex vivo permeation in human skin were evaluated. In vitro antimicrobial activity was studied using strains of C. albicans, C. glabrata and C. parapsilosis. The tolerability was evaluated using in vitro and in vivo models. AmB + BGEO gel presented appropriate characteristics for topical administration, including pH of 5.85, pseudoplastic behavior, optimal extensibility, as well as high stability and acceptable tolerability. In vitro release studies showed that the formulation releases the drug following a Boltzmann sigmoidal model. Finally, AmB + BGEO gel exhibited higher amount of drug retained inside the skin and lower Minimum Inhibitory Concentration than a formulation sans essential oil. Therefore, these results suggest that the incorporation of B. graveolens essential oil in the formulation could be used as strategy to promote a local effect in the treatment of cutaneous candidiasis.

scholarly journals Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 64 ◽  
Author(s):  
Lupe Carolina Espinoza ◽  
Marcelle Silva-Abreu ◽  
Beatriz Clares ◽  
María José Rodríguez-Lagunas ◽  
Lyda Halbaut ◽  
...  
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Release Profile ◽  
In Vivo Models ◽  
Tablet Form ◽  
Ex Vivo Permeation ◽  
Vitro Release

Donepezil (DPZ) is widely used in the treatment of Alzheimer’s disease in tablet form for oral administration. The pharmacological efficacy of this drug can be enhanced by the use of intranasal administration because this route makes bypassing the blood–brain barrier (BBB) possible. The aim of this study was to develop a nanoemulsion (NE) as well as a nanoemulsion with a combination of bioadhesion and penetration enhancing properties (PNE) in order to facilitate the transport of DPZ from nose-to-brain. Composition of NE was established using three pseudo-ternary diagrams and PNE was developed by incorporating Pluronic F-127 to the aqueous phase. Parameters such as physical properties, stability, in vitro release profile, and ex vivo permeation were determined for both formulations. The tolerability was evaluated by in vitro and in vivo models. DPZ-NE and DPZ-PNE were transparent, monophasic, homogeneous, and physically stable with droplets of nanometric size and spherical shape. DPZ-NE showed Newtonian behavior whereas a shear thinning (pseudoplastic) behavior was observed for DPZ-PNE. The release profile of both formulations followed a hyperbolic kinetic. The permeation and prediction parameters were significantly higher for DPZ-PNE, suggesting the use of polymers to be an effective strategy to improve the bioadhesion and penetration of the drug through nasal mucosa, which consequently increase its bioavailability.

PROPRANOLOL HYDROCHLORIDE TOPICAL GEL FOR THE TREATMENT OF INFANTILE HEMANGIOMA

2020 ◽  
pp. 143-150
Author(s):  
MANEESHA MURALI ◽  
SUJAID THAYYILAKANDY ◽  
MUHAMMED SHAFI P. A. ◽  
ARATHI VENU ◽  
SARITHA A. SURENDRAN ◽  
...  
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Infantile Hemangioma ◽  
Histopathological Study ◽  
Preliminary Evaluation ◽  
Propranolol Hydrochloride ◽  
Topical Gel ◽  
Skin Delivery ◽  
Vitro Release

Objective: To formulate and evaluate propranolol hydrochloride topical gel for overcoming the limitations and low oral bioavailability associated with conventional therapy. Methods: The propranolol hydrochloride topical gels were prepared by the cold mechanical method. The preliminary evaluation and further characterisation studies was conducted to find the optimised formulation. The in vitro release and ex vivo permeation studies were investigated. The histopathological studies and stability studies was also assessed. Results: The propranolol hydrochloride topical gel was successfully prepared. The in vitro release of optimized topical propranolol hydrochloride gel formulation (G2) showed the highest cumulative percentage drug release that is, 95.55%±0.15 after 7.5 h. (G2) the formulation showed a higher flux value of 4.61μg/cm2/h. The histopathological study using pig skin revealed that the optimized formulation was found to be safe for topical application. Conclusion: The formulated topical gel containing propranolol Hydrochloride seems to be a promising dosage form for enhanced skin delivery of propranolol hydrochloride in treating Infantile Hemangioma.

Sodium alginate nanoparticles as a new transdermal vehicle of glucosamine sulfate for treatment of osteoarthritis

2017 ◽  
Vol 9 (3-4) ◽  
Author(s):  
Asmaa S. El-Houssiny ◽  
Azza A. Ward ◽  
Dina M. Mostafa ◽  
Salwa L. Abd-El-Messieh ◽  
Kamal N. Abdel-Nour ◽  
...  
Keyword(s):  
Side Effects ◽  
Surface Charge ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Glucosamine Sulfate ◽  
Suspension Stability ◽  
Rat Skin ◽  
Release Studies ◽  
Vitro Release

AbstractGlucosamine sulfate (GS) has been used orally for the treatment of osteoarthritis (OA). However, it may be susceptible to the liver first pass phenomenon, which greatly affects its bioavailability, in addition to its side effects on the gastrointestinal tract. Alginate nanoparticles (Alg NPs) were investigated as a new drug carrier for transdermal delivery of GS to improve its effectiveness and reduce side effects. GS-Alg NPs were characterized by encapsulation efficiency, NP yield, particle size and surface charge properties. The in vitro release studies of GS and the ex vivo permeability through rat skin were determined using a UV-Vis spectrophotometer. GS-Alg NPs are within the nanometer range of size. High negative surface charge values are obtained and indicate the high suspension stability of the prepared formulation. The in vitro release studies showed that GS is released from Alg NPs in a sustained and prolonged manner. The ex vivo permeability of GS through rat skin is enhanced significantly after encapsulation in the negatively charged Alg NPs. We successfully reported a highly stable nanoparticlulate system using Alg NPs that permits the encapsulation of GS for topical administration, overcoming the disadvantages of oral administration.

Nanostructured Lipid Carriers for Intranasal Administration of Olanzapine in the management of Schizophrenia

2021 ◽  
Vol 14 ◽  
Author(s):  
Sarbjot Kaur ◽  
Ujjwal Nautiyal ◽  
Pooja A. Chawla ◽  
Viney Chawla
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Nanostructured Lipid Carriers ◽  
Polydispersity Index ◽  
Poloxamer 407 ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
Vitro Release

Background: Background: Olanzapine belongs to a new class of dual spectrum antipsychotic agents. It is known to show promise in managing both the positive and negative symptoms of schizophrenia. Drug delivery systems based on nanostructured lipid carriers (NLC) are expected to provide rapid nose-to-brain transport of this drug and improved distribution into and within the brain. Objective: The present study deals with the preparation and evaluation of olanzapine loaded NLC via the intranasal route for schizophrenia. Methods: Olanzapine-NLC were formulated through the solvent injection method using isopropyl alcohol as the solvent, stearic acid as solid lipid, and oleic acid as liquid lipid, chitosan as a coating agent, and Poloxamer 407 as a surfactant. NLC were characterized for particle size, polydispersity index, entrapment efficiency, pH, viscosity, X-ray diffraction studies, in-vitro mucoadhesion study, in- vitro release and ex-vivo permeation studies. The shape and surface morphology of the prepared NLC was determined through transmission electron microscopy. To detect the interaction of the drug with carriers, compatibility studies were also carried out. Results: Average size and polydispersity index of developed formulation S6 was 227.0±6.3 nm and 0.460 respectively. The encapsulation efficiency of formulation S6 was found to be 87.25 %. The pH, viscosity, in-vitro mucoadhesion study, and in- vitro release of optimized olanzapine loaded NLC were recorded as 5.7 ± 0.05, 78 centipoise, 15±2 min, and 91.96 % respectively. In ex-vivo permeation studies, the percent drug permeated after 210 min was found to be 84.03%. Conclusion: These results reveal potential application of novel olanzapine-NLC in intranasal drug delivery system for treatment of schizophrenia.

Evaluation of the in vitro release and permeation of Cordia verbenacea DC essential oil from topical dosage forms

2019 ◽  
Vol 53 ◽  
pp. 101173 ◽  
Author(s):  
Jéssica Domingos da Silva ◽  
Márcio Vinícius Gomes ◽  
Lucio Mendes Cabral ◽  
Valeria Pereira de Sousa
Keyword(s):  
Essential Oil ◽  
In Vitro Release ◽  
Dosage Forms ◽  
Topical Dosage ◽  
Vitro Release ◽  
Topical Dosage Forms

scholarly journals SOLUBILITY ENHANCEMENT OF CELECOXIB BY SOLID DISPERSION TECHNIQUE AND INCORPORATION INTO TOPICAL GEL

2019 ◽  
pp. 294-300
Author(s):  
AMRIN SHAIKH ◽  
PRASHANT BHIDE ◽  
REESHWA NACHINOLKAR
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
In Vitro Drug Release ◽  
Peg 6000 ◽  
Topical Gel ◽  
Drug Content ◽  
Vitro Release

Objective: The aim of the present investigation was to design gels for the topical delivery of celecoxib and evaluate with an aim to increase its penetration through the skin and thereby its flux. Method: The solubility of celecoxib is shown to be increased by preparing solid dispersions (SDs) using carriers such as mannitol, polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG) 6000 and urea by solvent evaporation, fusion, and coevaporation methods. In vitro release profile of all SD was comparatively evaluated and studied against the pure drug. The prepared SD was subjected for percent practical yield, drug content, infrared spectroscopy, differential scanning calorimetry analysis, X-ray diffraction studies, and scanning electron microscopy (SEM) imaging. The celecoxib gel was prepared using hydroxypropyl methyl cellulose (HPMC) and Carbopol containing a permeation enhancer dimethyl sulfoxide (DMSO) at different proportions and evaluated for drug content, pH, viscosity, spreadability, extrudability, stability, and in vitro drug release. Results: Faster dissolution rate was exhibited by SD containing 1:5 ratio of celecoxib: PVP K-30 prepared by coevaporation method. In vitro drug release of celecoxib, gels revealed that formulation with HPMC has higher drug release as compared to Carbopol. Conclusion: The increase in dissolution rate for SD is observed in the following order of PVP K-30>urea>mannitol>PEG 6000. The CPD5 gel containing a SD CP5 and 20% DMSO showed the best in vitro release 74.13% at the end of 6 h.

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