scholarly journals Formulation Development, Characterization and Antifungal Evaluation of Chitosan NPs for Topical Delivery of Voriconazole In Vitro and Ex Vivo

Polymers ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 135
Author(s):  
Muhammad Khurshid Alam Shah ◽  
Abul Kalam Azad ◽  
Asif Nawaz ◽  
Shafi Ullah ◽  
Muhammad Shahid Latif ◽  
...  
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Control Release ◽  
Topical Delivery ◽  
Tween 20 ◽  
Lauryl Sulfate ◽  
Formulation Development ◽  
Drug Content ◽  
Vitro Release

This study aims to develop chitosan-based voriconazole nanoparticles (NPs) using spray-drying technique. The effect of surfactants and polymers on the physicochemical properties, in vitro release, and permeation of NPs was investigated. The prepared NPs containing various surfactants and polymers (e.g., Tween 20 (T20), Tween 80 (T80), sodium lauryl sulfate (SLS), propylene glycol (PG), and Polyethylene glycol-4000 (PEG-4000)) were physiochemically evaluated for size, zeta potential, drug content, percent entrapment efficiency, in vitro release, and permeation across rats’ skin. A Franz diffusion cell was used for evaluating the in vitro release and permeation profile. The voriconazole-loaded NPs were investigated for antifungal activity against Candida albicans (C. albicans). The prepared NPs were in the nano range (i.e., 160–500 nm) and positively charged. Images taken by a scanning electron microscope showed that all prepared NPs were spherical and smooth. The drug content of NPs ranged from 75% to 90%. Nanoparticle formulations exhibited a good in vitro release profile and transport voriconazole across the rat’s skin in a slow control release manner. The NPs containing SLS, T80, and PG exhibited the best penetration and skin retention profile. In addition, the formulation exhibited a potential antifungal effect against C. albicans. It was concluded that the development of chitosan NPs has a great potential for the topical delivery of voriconazole against fungal infection.

scholarly journals FORMULATION DEVELOPMENT, EVALUATION AND OPTIMIZATION OF MEDICATED LIP ROUGE CONTAINING NIOSOMAL ACYCLOVIR FOR THE MANAGEMENT OF RECURRENT HERPES LABIALIS

2017 ◽  
Vol 9 (6) ◽  
pp. 21 ◽  
Author(s):  
Rajalakshmi S. V. ◽  
Vinaya O. G.
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Profile ◽  
Herpes Labialis ◽  
Formulation Development ◽  
Recurrent Herpes ◽  
Vitro Release

Objective: Aim of the study was to formulate, evaluate and optimize medicated Lip rouge containing acyclovir encapsulated inside a novel vesicular carrier, niosome so that the formulation can improve its membrane penetration. Formulating as a cosmetic Lip rouge formulation will also improve patient compliance in the treatment of herpes labialis.Methods: Acyclovir niosomes were prepared by thin film hydration method. Niosomes were evaluated and were optimized by considering the entrapment efficiency and in vitro release profile. The optimized niosomes were incorporated into lipstick, lip balm and lip rouge for selecting the best lip formulation. Based on the in vitro release profile, ease of application and properties of prepared formulations lip rouge was selected and further evaluations were carried out.Results: Among the six formulations of niosomes NF2 has showed 88.49 % entrapment efficiency and 86.97% cumulative drug release in 8 h. The formulation was optimized considering both entrapment efficiency and in vitro release. The optimized formulation of niosomes was incorporated into Lipstick, lip balm and lip rouge. The evaluation results of lipstick, lip balm and lip rouge for in vitro release suggested lip rouge as the best formulation. The percentage cumulative release of drug from optimized lip rouge at the end of 8 h was 84.77%. The percentage cumulative drug release in ex vivo studies for 8 h was 60.88 %.Conclusion: The results suggested that prepared lip rouge containing acyclovir niosomes can effectively deliver the drug than the marketed acyclovir cream and successful therapy of Recurrent Herpes labialis can be achieved.

scholarly journals The Effect of Acid Modification of Porcine Mucin on Its Drug Release and Skin Permeation Properties in Insulin Transdermal Films

2021 ◽  
Author(s):  
Sylvester O. Eraga ◽  
Matthew I. Arhewoh ◽  
Magnus A. Iwuagwu
Keyword(s):  
Blood Glucose ◽  
Moisture Content ◽  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Glucose Lowering ◽  
Drug Content ◽  
Folding Endurance ◽  
Vitro Release

Background: The transdermal delivery of insulin involving the use of polymers has been extensively reported. More recently, the use of mucoadhesive or bioadhesive polymers as an insulin base in its formulation is gaining attention possibly due to the penetration enhancing properties of the polymers. Objectives: This study aimed at determining the effect of acid-modified porcine mucin powder on the release and permeation of insulin in transdermal films. Methods: Various batches of insulin films were prepared by solvent casting method using polysorbate 80 as an emulsifying agent and acid-treated and untreated mucin powders as a base. The films were evaluated for their physical properties, folding endurance, moisture content and uptake, drug content, bioadhesion, in vitro release, ex vivo permeation, and in vivo glucose-lowering activity. Results: The prepared insulin films had a weight range of 0.21-0.27 g, folding endurance of 101-103, moisture content and uptake of 13.73%-18.57% and 11.70%-22.30%, respectively, and drug content of 96%-101%. The bioadhesion of the films prepared with acid-treated mucin was within the range of 0.088-0.186 Nm-1 as against 0.055 Nm-1 of the films prepared with untreated mucin. The in vitro release profiles showed a release of 95% insulin from films prepared with untreated mucin within 2 h while the films made with acid-treated mucin gave a release of about 60%-73% over the same period, indicating a slower release. Animals that received acid-treated mucin-base insulin films showed delayed but sustained blood-glucose-lowering up to 70% and for films prepared with untreated mucin 55% within 12 h.  Conclusion: Insulin transdermal films prepared with acid-modified mucin powder gave superior bioadhesive strength values. They also showed improved drug permeation enhancing ability and achieving up to 70% blood glucose lowering in diabetic rats.

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.

Chitosan (Poly-(D) glucosamine) based solid lipid nanoparticles of dexibuprofen for topical delivery: Formulation development and characterizations

2021 ◽  
pp. 1-12
Author(s):  
Irshadullah ◽  
Shefaat Ullah Shah ◽  
Muhammad Khalid Khan ◽  
Kifayat Ullah Shah ◽  
Barkat Ali Khan
Keyword(s):  
Surface Morphology ◽  
Solid Lipid Nanoparticles ◽  
Active Drug ◽  
In Vitro Release ◽  
Topical Delivery ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Permeation Study ◽  
Vitro Release

Chitosan a poly-(D) glucosamine is a polysaccharide made by treating shrimp and other crustacean shells with the alkali sodium hydroxide. It is a hydrophilic polymer that helps to retain the drug inside the solid lipid nanoparticles (SLN’s) and prolongs the release of drug from the carrier system. The purpose of the study was to formulate Chitosan decorated SLN’s for the topical delivery of dexibuprofen by hot pressure homogenization technique. Blank SLN’s, drug loaded SLN’s and Chitosan decorated SLN’s were prepared. Particle size, zeta potential and PDI were determined. FTIR study was conducted to evaluate the compatibility of excipients with the active drug. Surface morphology of SLN’s was determined by field emission scanning electron microscope. Drug content and entrapment efficiency of SLN’s were determined using indirect method. In vitro release and ex vivo permeation study of SLN’s were carried out using Franz diffusion cell. The droplet size fell into the nano range i.e. 132±7 to 424±2 nm which is effective for topical drug delivery system. The PDI of formulations range from 0.21 to 0.42 which depicts the homogeneity of all the SLN’s formulations. Vibrational analysis indicates that there is no interaction between active drug and excipient used in the formulation. The surface morphology revealed the spherical shape of Chitosan decorated SLN’s. The in vitro release of formulations showed 79.91±1.07 to 89.94±1.8 % drug release. The drug permeation study showed high permeation of drug into the skin. The percent drug permeation ranges from 64.15±0.93 to 71.80±0.88% indicating good permeation of drug across the skin. Overall, SLN’s are an effective carrier for topical delivery of dexibuprofen and thus bypasses side effects associated with oral delivery.

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.

scholarly journals Design and evaluation of Pulsatile drug delivery of Losartan Potassium

2014 ◽  
Vol 12 (2) ◽  
pp. 119-123
Author(s):  
MS Ashwini ◽  
Mohammed Gulzar Ahmed
Keyword(s):  
In Vitro Release ◽  
Losartan Potassium ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Weight Variation ◽  
Release Studies ◽  
The Stability ◽  
Vitro Release

The study was designed for the investigation of pulsatile device to achieve time or site specific release of Losartan potassium based on chronopharmaceutical considerations. The basic design involves the preparation of cross linked hard gelatin capsules by using formaldehyde, then the drug diluent mixture were prepared and loaded in, which was separated by using hydrogel plugs of different polymers of different viscosities. Prepared formulations were subjected to evaluation of various parameters like weight variation, percentage drug content, in vitro drug release and stability studies. Weight variation and percentage drug content results showed that they were within the limits of official standards. The in-vitro release studies revealed that the capsules plugged with polymer HPMC showed better pulsatile or sustained release property as compared to the other formulations. The stability studies were carried out for all the formulations and formulations F1 & F2 were found to be stable. Dhaka Univ. J. Pharm. Sci. 12(2): 119-123, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17610

scholarly journals FORMULATION OF POLYMERIC NANOSUSPENSION CONTAINING PRAMIPEXOLE DIHYDROCHLORIDE AND HESPERIDIN FOR IMPROVED TREATMENT OF PARKINSON’S DISEASES

2018 ◽  
Vol 11 ◽  
Author(s):  
Somasundaram I
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Drug Content ◽  
Pramipexole Dihydrochloride ◽  
Vitro Release

Aims and Objectives: The present study is to formulate the nanosuspension containing a hydrophilic drug pramipexole dihydrochloride and hesperidin and to increase the drug entrapment efficiency.Methods: Hesperidin and pramipexole dihydrochloride loaded in chitosan nanosuspension is prepared by ionic gelation method using chitosan and tripolyphosphate. There was no incompatibility observed between the drug and polymer through Fourier transform infrared and differential scanning calorimetric. Various other parameters such as particle size, zeta potential, scanning electron microscope, drug content, drug entrapment efficiency, and in vitro release have been utilized for the characterization of nanoparticles.Results and Discussion: The average size of particle is 188 nm; zeta potential is 46.7 mV; drug content of 0.364±0.25 mg/ml; entrapment efficiency of 72.8% is obtained with HPN3 formulation. The PHC1 shows the highest drug release followed by PHC2 due to low concentration of polymer and PHC4 and PHC5 show less drug release due to high concentration of polymer. The in vitro release of PHC3 is 85.2%, initial the burst release is shown which is approximately 60% in 8 h; then, slow release later on drastic reduction in release rate is shown in 24 h. The in vivo study histopathological report confers the effective protective against rotenone induces Parkinson’s.Conclusion: PHC3 was chosen as the best formulation due to its reduced particle size and controlled release at optimum polymer concentration which may be used to treat Parkinson’s disease effectively..

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