Multiunit floating drug delivery system of acyclovir: development, characterization and in vitro-in vivo evaluation of spray-dried hollow microspheres

Bhosale, U.V.; Devi, Kshama; Choudhary, Sandeep

doi:10.1016/s1773-2247(12)50095-x

Cited by 6 publications

(5 citation statements)

References 15 publications

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“… Drug name Fabrication Duration of release (h) Antibacterial activity Animal study Ref. Azithromycin Nanoformulation 24 – In vivo (mice) 56 Azithromycin Niosomal gel 24 Staphylococcus aureus Staphylococcus epidermidis Ex vivo (rat abdominal skin) 57 Vancomycin Transferosome 24 – Ex vivo (wistar rat skin) 58 Azithromycin Hollow microsphere 12 – In vivo (rabbit) 59 Azithromycin Phase inversion 240 Streptococcus sobrinus Escherichia coli Pseudomonas aeruginosa Staphylococcus aureus Ex vivo (mice skin) This study …”

Section: Resultsmentioning

confidence: 99%

Designing of a new transdermal antibiotic delivery polymeric membrane modified by functionalized SBA-15 mesoporous filler

Samari,

Kashanian,

Zinadini

et al. 2024

Sci Rep

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A new drug delivery system using an asymmetric polyethersulfone (PES) membrane modified by SBA-15 and glutamine-modified SBA-15 (SBA-Q) was prepared in this study by the aim of azithromycin delivery enhancement in both in vitro and ex vivo experiments. The research focused on optimizing membrane performance by adjusting critical parameters including drug concentration, membrane thickness, modifier percentage, polymer percentage, and pore maker percentage. To characterize the fabricated membranes, various techniques were employed, including scanning electron microscopy, water contact angle, and tensile strength assessments. Following optimization, membrane composition of 17% PES, 2% polyvinylpyrrolidone, 1% SBA-15, and 0.5% SBA-Q emerged as the most effective. The optimized membranes demonstrated a substantial increase in drug release (906 mg/L) compared to the unmodified membrane (440 mg/L). The unique membrane structure, with a dense top layer facilitating sustained drug release and a porous sub-layer acting as a drug reservoir, contributed to this improvement. Biocompatibility assessments, antibacterial activity analysis, blood compatibility tests, and post-diffusion tissue integrity evaluations confirmed the promising biocompatibility of the optimized membranes. Moreover, long-term performance evaluations involving ten repeated usages underscored the reusability of the optimized membrane, highlighting its potential for sustained and reliable drug delivery applications.

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Section: Resultsmentioning

confidence: 99%

Designing of a new transdermal antibiotic delivery polymeric membrane modified by functionalized SBA-15 mesoporous filler

Samari,

Kashanian,

Zinadini

et al. 2024

Sci Rep

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“…The results showed it improved two to three folds in the oral bioavailability of acyclovir. 32 Another study also indicated riboflavin-loaded microballoons as a floating controlled drug delivery system were very useful for improving oral drug bioavailability in healthy humans. 33 …”

Section: Resultsmentioning

confidence: 99%

A 5-fluorouracil-loaded floating gastroretentive hollow microsphere: development, pharmacokinetic in rabbits, and biodistribution in tumor-bearing mice

Huang¹,

Wei²,

Yang³

et al. 2016

DDDT

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5-Fluorouracil (5-FU) was loaded in hollow microspheres to improve its oral bioavailability. 5-FU hollow microspheres were developed by a solvent diffusion–evaporation method. The effect of Span 80 concentration, ether/ethanol volume ratio, and polyvinyl pyrrolidone/ethyl cellulose weight ratio on physicochemical characteristics, floating, and in vitro release behaviors of 5-FU hollow microspheres was investigated and optimized. The formulation and technology composed of Span 80 (1.5%, w/v), ether/ethanol (1.0:10.0, v/v), and polyvinyl pyrrolidone/ethyl cellulose (1.0:10.0, w/w) were employed to develop three batch samples, which showed an excellent reproducibility. The microspheres were spherical with a hollow structure with high drug loading amount (28.4%±0.5%) and production yield (74.2%±0.6%); they exhibited excellent floating and sustained release characteristics in simulated gastric and intestinal fluid. Pharmacokinetic studies demonstrated that 5-FU hollow microspheres significantly enhanced oral bioavailability (area under curve, [AUC](0−t): 12.53±1.65 mg/L*h vs 7.80±0.83 and 5.82±0.83 mg/L*h) with longer elimination half-life (t1/2) (15.43±2.12 hours vs 2.25±0.22 and 1.43±0.18 hours) and mean residence time (7.65±0.97 hours vs 3.61±0.41 and 2.34±0.35 hours), in comparison with its solid microspheres and powder. In vivo distribution results from tumor-bearing nude mice demonstrated that the animals administered with 5-FU hollow microspheres had much higher drug content in tumor, plasma, and stomach at 1 and 8 hours except for 0.5 hours sample collection time point in comparison with those administered with 5-FU solid microspheres and its powder. These results suggested that the hollow microspheres would be a promising controlled drug delivery system for an oral chemotherapy agent like 5-FU.

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“…Acyclovir [9-(2-hydroxyethoxymethyl) guanine] (ACV), is a synthetic purine nucleoside analog derived from guanine 9,10 which is considered as the first agent to be licensed for the treatment of herpes simplex virus (HSV-1, HSV-2) infections and is the most widely used drug for infections such as cutaneous herpes, genital herpes, chicken pox, varicella zoster infections through interfering with DNA synthesis and inhibiting viral replication. [11][12][13] According to the Biopharmaceutical Classification System (BCS), ACV falls under the BCS Class III drug i.e. soluble with low intestinal permeability and needs to be administered in large doses orally or intravenously to obtain the desired therapeutic effect.…”

Section: Introductionmentioning

confidence: 99%

“…Furthermore, because the mean plasma half-life of the drug is 2.5 h, five times a day administration is required which causes compliance problems to patients. 11,15 Therefore, the aim of the study was to develop mucoadhesive sustained-release formulations of ACV in the form of microspheres using BBD in combination with a desirability function and to evaluate the main effects of formulation variables on three responses: cumulative percentage of drug release at 8 hour, bond strength and swelling at 4 hour.…”

Section: Introductionmentioning

confidence: 99%

Development and Optimization of Acyclovir Loaded Mucoadhesive Microspheres by Box – Behnken Design

Karmoker

Hasan

Ahmed

et al. 2019

Dhaka Univ. J. Pharm. Sci

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The grail of the study was to design, develop and characterize sustained release mucoadhesive microspheres of acyclovir and to optimize the drug release profile using response surface methodology by applying Box–Behnken design (BBD) which was equipped with three levels and three factors. Microspheres were prepared from Methocel K15M and Ethocel Standard 45 Premium using the emulsification solvent evaporation technique. The independent factors were the amounts of Methocel K15M (X1), amount of Ethocel Standard 45 Premium (X2), and RPM (X3). The dependent variables were cumulative percentage drug release (CDR) at 8 hour (Y1), bond strength (Y2), and swelling at 4 hour (Y3). To understand the effects of different factor level combinations on the responses, various response surface graphs and contour plots were prepared. Predicted values and experimental values for optimized formulation (X1 = 600 mg, X2 = 500 mg, and X3 = 336.57) was found to be in close agreement. Dhaka Univ. J. Pharm. Sci. 18(1): 1-2, 2019 (June)

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Multiunit floating drug delivery system of acyclovir: development, characterization and in vitro-in vivo evaluation of spray-dried hollow microspheres

Cited by 6 publications

References 15 publications

Designing of a new transdermal antibiotic delivery polymeric membrane modified by functionalized SBA-15 mesoporous filler

Designing of a new transdermal antibiotic delivery polymeric membrane modified by functionalized SBA-15 mesoporous filler

A 5-fluorouracil-loaded floating gastroretentive hollow microsphere: development, pharmacokinetic in rabbits, and biodistribution in tumor-bearing mice

Development and Optimization of Acyclovir Loaded Mucoadhesive Microspheres by Box – Behnken Design

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