Impact of the mucoadhesive lyophilized wafer loaded with novel carvedilol nano-spanlastics on biochemical markers in the heart of spontaneously hypertensive rat models

Sallam, Nahed Mohamed; sanad, rania; Ahmed, Mahgoub M; Khafagy, El-Sayed; Ghorab, Mostafa M.; Gad, Shadeed

doi:10.1007/s13346-020-00814-4

Cited by 31 publications

(15 citation statements)

References 55 publications

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“…It was also observed that the prepared bilosomes confirmed satisfactory ZP values around ±30 mV that confirm their stability due to electrical repulsion between particles [31] [6] [30].…”

Section: Physical Characterization Of Bilosomesmentioning

confidence: 64%

‘Preparation and characterization of a novel mucoadhesive carvedilol nano-sponge: a promising platform for buccal antihypertensive delivery’

Sallam

Sanad

Ahmed

et al. 2021

Preprint

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Purpose: Carvedilol (CRV) is a non-selective beta-blocker used for hypertension treatment, angina pectoris, and heart failure. Oral administration of CRV showed poor bioavailability (25%), which may be due to exposure to the first-pass metabolism. Buccal delivery was used to boost its bioavailability.Methods: In this study carboxymethylcellulose/hydroxypropyl cellulose (CMC/HPC) composite buccal sponge enriched with CRV bilosomes was developed. Bilosomes were prepared using the thin-film hydration-sonication technique by applying a 32 -factorial design.Results: BL9 possessed the highest desirability value (0.861) and therefore, it was chosen as an optimal bilosomes. It exhibited a spherical shape with 217.2 nm, 87.13% entrapment efficiency, and a sustained release of CRV up to 24h. Consecutively, BL9 was incorporated in a CMC/HPC gel and lyophilized for 24 h to obtain a CMC-HPCL9 bilosomal sponge to enhance CRV buccal delivery. Morphological analysis of the prepared sponge with improved swelling showed a porosity of 67.58 percent. The in vivo assessment of rats indicates that the CMC-HPC/BL9 sponge enhances systolic/diastolic blood pressure, lipid profiles, oxidative stress biomarkers, and heart biomarkers with improved heart tissue quality.Conclusion: These results strongly encourage the use of this novel CMC-HPC/BL9 composite buccal sponge for the management of hypertension.

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“…It was also observed that the prepared bilosomes confirmed satisfactory ZP values around ±30 mV that confirm their stability due to electrical repulsion between particles [31] [6] [30].…”

Section: Physical Characterization Of Bilosomesmentioning

confidence: 64%

‘Preparation and characterization of a novel mucoadhesive carvedilol nano-sponge: a promising platform for buccal antihypertensive delivery’

Sallam

Sanad

Ahmed

et al. 2021

Preprint

Self Cite

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“…Ethanol injection method was employed to prepare spanlastics dispersions loaded with LAA as previously described by Sallam et al. ( 2020 ). In brief, LAA and span were dissolved together in ethanol kept at 50 °C, the solution was then injected slowly into preheated aqueous solution (60 °C) containing an edge activator (EA).…”

Section: Methodsmentioning

confidence: 99%

“…Spanlastics are classified as ultra-deformable or elastic vesicles (Sallam et al. 2020 ). Unlike liposomes and niosomes, spanlastics contain surfactants in their composition employed as edge activators for destabilization of the lipid bilayer thus increasing its deformability and enhancing percutaneous absorption of drugs (Doppalapudi et al.…”

Section: Introductionmentioning

confidence: 99%

Topical delivery of l -ascorbic acid spanlastics for stability enhancement and treatment of UVB induced damaged skin

2021

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l -Ascorbic acid (LAA) is considered a powerful antioxidant that protects skin from premature aging. Maintaining the stability of vitamin C remains the biggest challenge in cosmeceuticals. Our main aim is the entrapment of high dose of vitamin C in spanlastic vesicles to provide maximum stability and efficacy. LAA-loaded spanlastics were prepared by ethanol injection method and were characterized for entrapment efficiency (EE%), particles size (PS), polydispersity index (PDI), zeta potential, deformability index (DI) and in vivo skin permeation. Selected spanlastics formula composed of span 60 and tween 60 (5:1) showed highest EE% of 89.77 ± 3.61% (w/w), high deformability of 11.13 ± 1.145 as well as good physical and chemical stability for 6 months. Improved drug penetration into stratum corneum (SC) was obtained from spanlastics compared to topical LAA solution. Quantitative real time PCR revealed that MMP2 and MMP9 levels were significantly suppressed in response to LAA spanlastics treated rats by 30.4% and 65.3%, respectively, when compared to the control group after exposure to UV irradiation. Results were confirmed by western blot analysis. Histopathological study of rat skin after UV irradiation revealed that application of LAA-loaded spanlastics provided the highest skin protection compared to UVB and LAA solution treated group which was evident by the normal thick epidermal morphology and the densely arranged dermal collagen fibers. LAA-loaded spanlastics successfully improved LAA stability, skin permeation and antioxidant protection against skin photodamage.

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“…The sublingual mucosa was carefully removed from heads of Rahmani sheep and soaked in phosphate buffer saline (PBS) pH 6.8 and instantly frozen at −80 °C until being used. Directly before the experiment, the mucosa was thawed and suspended in PBS (pH 6.8) for 30 min to equilibrate (Sallam et al, 2020 ). Using modified dissolution apparatus (Hanson Research dissolution apparatus, Frankfurt, Germany) in which buccal mucosa was cut and mounted on the bottom of a cylindrical plastic support (of area 1.766 cm 2 ) connected to the drive shaft of the dissolution apparatus.…”

Section: Methodsmentioning

confidence: 99%

Formulation, characterization, optimization, and in-vivo performance of febuxostat self-nano-emulsifying system loaded sublingual films

et al. 2021

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Febuxostat (FXS) is a potent antigout drug with poor water solubility and relative high first-pass effect leading to moderate oral bioavailability (<49%). This study aimed to increase FXS solubility and bioavailability by optimizing sublingual fast-dissolving films (SFs) containing a selected FXS self-nanoemulsifying system (s-SNES) previously prepared by our team. The s-SNES was loaded into SFs by solvent casting technique. A full factorial design (3 2 ) was applied to study the effects of polymer and plasticizer types on mechanical characteristics and the dissolution profile of FXS from the SFs. Numerical optimization was performed to select the SF having highest desirability according to predetermined characteristics. The optimized SF (O-SF) contained 1 g of s-SNES, polyvinylpyrrolidone K30 (6%w/v), polyethylene glycol 300 (20%w/w of polymer wt.), and Avicel PH101 (0.5%w/v). O-SF showed good permeation of FXS through sheep sublingual tissue. Storage of O-SF for three months showed no significant change in the FXS dissolution profile. In-vivo performance of O-SF in rabbits was compared to that of oral marketed tablets (Staturic V R 80 mg). A cross-over design was applied and pharmacokinetic parameters were calculated after ensuring absence of sequence effect. Statistical analysis revealed better performance for O-SF with significantly higher C max , AUC 0-24 , AUC 0-1 , apparent t 1/2 together with lower t max , and apparent k el than marketed tablets. Relative bioavailability of O-SF compared to the marketed tablet was found to be 240.6%. This confirms the achievement of the study aims of improving dissolution rate and bioavailability of FXS using a patient-wise convenient formula.

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Impact of the mucoadhesive lyophilized wafer loaded with novel carvedilol nano-spanlastics on biochemical markers in the heart of spontaneously hypertensive rat models

Cited by 31 publications

References 55 publications

‘Preparation and characterization of a novel mucoadhesive carvedilol nano-sponge: a promising platform for buccal antihypertensive delivery’

‘Preparation and characterization of a novel mucoadhesive carvedilol nano-sponge: a promising platform for buccal antihypertensive delivery’

Topical delivery of l -ascorbic acid spanlastics for stability enhancement and treatment of UVB induced damaged skin

Formulation, characterization, optimization, and in-vivo performance of febuxostat self-nano-emulsifying system loaded sublingual films

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