scholarly journals Influence of Lactobacillus Biosurfactants on Skin Permeation of Hydrocortisone

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 820
Author(s):  
Angela Abruzzo ◽  
Carola Parolin ◽  
Elisa Corazza ◽  
Barbara Giordani ◽  
Massimiliano Pio di Cagno ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Aqueous Solubility ◽  
Skin Hydration ◽  
Permeation Enhancers ◽  
Scanning Calorimetry ◽  
Drug Permeation ◽  
Diffusion Studies ◽  
Model Drug ◽  
Dsc Curves

One of the most widely used strategies to improve drug diffusion through the skin is the use of permeation enhancers. The aim of this work was to investigate the effect of two biosurfactants (BS), produced by Lactobacillus crispatus BC1 and Lactobacillus gasseri BC9, on the skin permeation profile of hydrocortisone (HC, model drug). HC aqueous solubility and in vitro diffusion studies through porcine skin were performed in the presence of BC1-BS and BC9-BS at concentrations below and above critical micellar concentrations (CMC). Moreover, skin hydration tests and differential scanning calorimetry (DSC) analysis were performed to further investigate BS interaction with the outermost layer of the skin. Both BS increased HC solubility, especially at concentrations above their CMC. At concentrations below the CMC, drug permeation through the skin was improved, as the result of a dual effect: a) the formation of a superficial lipophilic environment, as confirmed by the reduction in skin hydration and b) the interaction between BS and the stratum corneum (SC), as demonstrated by the DSC curves. From the obtained data, it appears that BC1-BS and BC9-BS could represent new promising green excipients for drug permeation enhancement through the skin.

DESIGN AND EVALUATION OF CHITOSAN-HPMC POLYMERIC FILMS FOR TRANSDERMAL DELIVERY OF CAPTOPRIL

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (06) ◽  
pp. 69-72
Author(s):  
Rajesh Sreedharan Nair ◽  
Manickam Balamurugan ◽  
Meng Sheng Teng
Keyword(s):  
Transdermal Delivery ◽  
Moisture Absorption ◽  
Hydroxypropyl Methylcellulose ◽  
Physicochemical Characterization ◽  
Scanning Calorimetry ◽  
Drug Permeation ◽  
Evaporation Technique ◽  
Model Drug ◽  
The Stability

Drug permeation through the skin layers remains a major challenge in transdermal drug delivery. In this study, the permeation enhancing property of chitosan together with its rate-controlling property has been utilized in the development of an efficient transdermal delivery system, using captopril as a model drug. Chitosan-hydroxypropyl methylcellulose (HPMC) films were developed by solvent evaporation technique. The films were characterized for appearance, thickness, weight uniformity, drug content, folding endurance and moisture absorption. Drug-polymer interaction was assessed using ATR-FTIR spectroscopy and Differential Scanning Calorimetry. The in vitro permeation carried out in Franz-type diffusion cells using synthetic Strat-M® membrane, demonstrated that the film coded F2 (Chitosan:HPMC = 50:50) showed a significant increase in drug permeation than F1 (Chitosan:HPMC = 90:10) with a flux value 86.7 µg/cm2/h. The physicochemical characterization and the stability studies confirmed that the formulated films were chemically and physically stable.

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

scholarly journals Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy

Polymers ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 923
Author(s):  
Shadab Md ◽  
Nabil A. Alhakamy ◽  
Hibah M. Aldawsari ◽  
Mohammad Husain ◽  
Nazia Khan ◽  
...  
Keyword(s):  
Skin Cancer ◽  
Zeta Potential ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Skin Layer ◽  
Vesicle Size ◽  
Cytotoxicity Activities

Plumbagin (PLM) is a phytochemical which has shown cytotoxicity against of cancer cells both in vitro and in vivo. However, the clinical application of PLM has been hindered due to poor aqueous solubility and low bioavailability. The aim of the present study was to develop, optimize and evaluate PLM-loaded glycerosome (GM) gel and compare with conventional liposome (CL) for therapeutic efficacy against skin cancer. The GM formulations were optimized by employing design expert software by 3-level 3-factor design. The prepared GMs were characterized in vitro for vesicle size, size distribution, zeta potential, vesicle deformability, drug release, skin permeation, retention, texture, antioxidant and cytotoxicity activities. The optimized formulation showed a vesicle size of 119.20 ± 15.67 nm with a polydispersity index (PDI) of 0.145 ± 0.02, the zeta potential of −27 ± 5.12 mV and entrapment efficiency of 76.42 ± 9.98%. The optimized PLM-loaded GM formulation was transformed into a pre-formed gel which was prepared using Carbopol 934 polymer. The drug diffusion fluxes of CL gel and GM-loaded gel were 23.31 ±6.0 and 79.43 ± 12.43 µg/ cm2/h, respectively. The result of texture analysis revealed the adequate hardness, cohesiveness, consistency, and viscosity of the developed GM-loaded gel compared to CL gel. The confocal images showed that glycerosomal gel has deeper skin layer penetration as compared to the control solution. GM-loaded gel treated rat skin showed significantly (p < 0.05) higher drug accumulation in the dermis, higher cytotoxicity and higher antioxidant activity as compared to CL gel and PLM suspension. Thus, findings revealed that novel GM-loaded gel could be potential carriers for therapeutic intervention in skin cancer.

scholarly journals PREPARATION AND CHARACTERIZATION OF NANOCRYSTALS FOR SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF PALIPERIDONE USING DIFFERENT HYDROPHILIC CARRIERS: IN VITRO-IN VIVO STUDY

2018 ◽  
Vol 11 (4) ◽  
pp. 393
Author(s):  
Moon Rajkumar ◽  
Gattani Surendra
Keyword(s):  
Dissolution Rate ◽  
Antipsychotic Agent ◽  
Aqueous Solubility ◽  
In Vivo Study ◽  
Scanning Calorimetry ◽  
Antisolvent Precipitation ◽  
Enhanced Solubility ◽  
Pure Drug

 Objective: The objective of this study was to increase the solubility and dissolution rate of paliperidone (PAL) by preparing its nanocrystals using different hydrophilic carriers by antisolvent precipitation technique.Methods: The nanoparticles (NP) were characterized for aqueous solubility, drug content, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, particle size, and in vitro-in vivo analysis.Results: The results showed improved solubility and dissolution rate of NPs when compared to pure drug and physical mixture (PM). Solubility data showed a linear graph giving an indication that there is a gradual increase in the solubility profile of the drug with an increase in concentration of the carriers. At highest concentration, the solubility of NPs with Plasdone S630, Povidone K-25, and PVP K-30 found to be increased by 12 folds, 9 folds and 6 folds, respectively, as compared to pure drug. The release profile of NPs with Plasdone S630 in terms of dissolution efficiency at 60 min (DE60), initial dissolution rate (IDR), amount release in 15 min (Q15 min), and time for 75% release (t75%) shows better results when compared to pure drug, PM, and also NPs with povidone 25 and povidone 30. In vivo study reveals that optimized NPs elicited significant induction of cataleptic behavior which is the indication of antipsychotic agent(s) effect.Conclusion: The process antisolvent precipitation under constant stirring may be a promising method to produce stable PAL NPs with markedly enhanced solubility and dissolution rate due to nanonization with the increased surface area, improved wettability, and reduced diffusion pathway.

Influence of skin permeation enhancers on the transdermal delivery of palonosetron: An in vitro evaluation

2018 ◽  
Vol 16 (3) ◽  
pp. 192-197 ◽  
Author(s):  
Anroop B. Nair ◽  
Shery Jacob ◽  
Bandar E. Al-Dhubiab ◽  
Rakan Naser Alhumam
Keyword(s):  
Transdermal Delivery ◽  
Skin Permeation ◽  
Permeation Enhancers ◽  
In Vitro Evaluation

scholarly journals Hydrophilic Sugars for Enhancing Dissolution Rate of Cilostazol: Effect of Wet Co-Processing

2020 ◽  
Vol 27 (1) ◽  
pp. 111-120
Author(s):  
Alaa Yosf Bazeed ◽  
Ahmed Nouh ◽  
Ebtessam Ahmed Essa ◽  
Gamal El Maghraby
Keyword(s):  
Aqueous Solubility ◽  
Submicron Particles ◽  
Drug Dissolution ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Swallowing Difficulties ◽  
Fast Disintegrating Tablets

Background: Cilostazol is an anti-platelets drug with considerable antithrombotic effects in vivo. Therefore, it is widely used by elderly patients. However, it suffers from poor bioavailability due to its low aqueous solubility. The objective of this work was to enhance the dissolution of cilostazol with the aim of formulating fast dissolving tablets for geriatrics and those of swallowing difficulties. Methods: Ethanol-assisted co-grinding of cilostazol with sugar-based excipients was adopted. Sucralose and mannitol were used for this purpose as hydrophilic excipient as well as taste improving agents. The obtained products were investigated regarding differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction, scanning electron microscope (SEM) and in vitro drug dissolution. Fast disintegrating tablets were prepared and evaluated. Results: Thermal behavior of the developed products reflected reduced crystallinity, it also suggested possible existence of new crystalline species with sucralose. Eutexia was also suggested for mannitol mixtures, that was supported by X-ray diffraction data. SEM indicated size reduction with the deposition of the drug as submicron particles over the excipient surface. Co-processing markedly improved cilostazol dissolution compared to unprocessed drug. The optimized formulations were successively formulated into fast disintegrating tablets. Conclusion: This investigation introduced the wet grinding strategy with sugar excipients as a platform for the formulation of easy to use tablets with optimum drug release.

scholarly journals A stepwise protocol for drug permeation assessment that combines heat-separated porcine ear epidermis and vertical diffusion cells

2018 ◽  
Vol 72 (1) ◽  
pp. 47-53 ◽  
Author(s):  
Ivana Pantelic ◽  
Tanja Ilic ◽  
Bojan Markovic ◽  
Sanela Savic ◽  
Milica Lukic ◽  
...  
Keyword(s):  
Evaluation Method ◽  
In Vitro Test ◽  
Formulation Development ◽  
Vertical Diffusion ◽  
Synthetic Membranes ◽  
Drug Permeation ◽  
Diffusion Cells ◽  
Drug Sample ◽  
Model Drug

After decades long absence of an official consensus on the most appropriate evaluation method for in vitro skin performance of topical semisolid drugs, United States Pharmacopoeia (USP 39) finally suggested three types of testing equipment; however, all these provide data on drug release using inert synthetic membranes. Considering the need for a readily available membrane that would be more structurally similar to human skin, this paper provides a detailed protocol of a method for drug permeation assessment that uses heat-separated porcine ear epidermis and modified Franz diffusion cells. Phases that were shown to be critical for variability of the results are identified (e.g., membrane preparation), and process parameters optimized. Applicability of the method was tested on four cream samples loaded with aceclofenac as a model drug. Sample compositions were designed in such a way to provide ?large? variations (variation of the main stabilizer: natural-origin versus synthetic emulsifier) and relatively ?minor? variations (co-solvent variation: none/isopropanol/glycerol). The developed protocol is a straightforward and reliable in vitro test for the evaluation of rate and extent of drug delivery into/through the skin. Moreover, this protocol may be routinely applied even in averagely equipped laboratories during formulation development or preliminary bioequivalence assessment of generic topical semisolids.

scholarly journals Preparation and characterization of ϐlurbiprofen capsules prepared by using liquisolid technique

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 2966-2974
Author(s):  
Madhavi K ◽  
Neelesh M
Keyword(s):  
Aqueous Solubility ◽  
Dissolution Profile ◽  
Coating Materials ◽  
In Vitro Drug Release ◽  
Drug Concentrations ◽  
Liquid Medication ◽  
Release Studies ◽  
Model Drug

The current project is mainly focussed on the application of liquisolid (LS) technique in the enhancement of dissolution profile of flurbiprofen. Flurbiprofen is a NSAID indicated for acute and chronic osteoarthritis, rheumatoid arthritis and spondylitis. It is selected as model drug as it is a BCS Class II drug and has very poor aqueous solubility of 10.45 ± 3.2μg/ml. Hence, this study was designed to improve the dissolution rate of flurbiprofen using LS technique. Initially, saturation solubility studies were performed to select liquid vehicle showing higher solubility of drug to obtain liquid medication. PEG 600 was selected as non-volatile solvent, used at three different drug concentrations of 33.33, 40 and 50 % w/w to form LS formulations. Further, they were converted to powder by means of  Avicel PH 102 and Aerosil 200 as carrier and coating materials to prepare LS formulations. Rheological tests were performed for the LS powder systems to study the flow properties. Later, several LS formulations were prepared, encapsulated in hard gelatin capsules. These capsules containing LS systems were subjected to evaluation tests and in vitro drug release studies. The results of dissolution profile of formulation CF3 showed maximum release of 98% within 30 minutes which was two folds higher than that of conventional capsule. FTIR studies revealed no drug-excipient interaction. DSC, SEM and PXRD studies revealed that drug in the system was completely soluble and available in molecularly dispersed state. Finally, it can be concluded that LS technique proved to enhance the dissolution profile of Flurbiprofen. 

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