Formulation of Chitosan Polymeric Vesicles of Ciprofloxacin for Ocular Delivery: Box-Behnken Optimization, In Vitro Characterization, HET-CAM Irritation, and Antimicrobial Assessment

Ameeduzzafar,; Alruwaili, Nabil K.; Imam, Syed Sarim; Alotaibi, Nasser Hadal; Alhakamy, Nabil A.; Alharbi, Khalid Saad; Alshehri, Sultan; Afzal, Muhammad; Alenezi, Sattam Khulaif; Bukhari, Syed Nasir Abbas

doi:10.1208/s12249-020-01699-9

Cited by 40 publications

(8 citation statements)

References 41 publications

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“… 42 Noticeably, the size of the prepared chitosomes significantly (p<0.05) increased with the increment of CS concentration. 43 The most acceptable PS for mucoadhesion is 200–500 nm, 23 which precludes the use of C3 for this purpose. The increase in the ZP value of the C1 formulation to −4.71±0.67 indicates an incomplete formation of CS coating around vesicles; however, the attainment of positive charge for both C2 and C3 formulations (+28.1±0.10 and +30.33±1.72, respectively) implies efficient coating with CS cationic polymer.…”

Section: Resultsmentioning

confidence: 99%

Novel Mucoadhesive Chitosomes as a Platform for Enhanced Oral Bioavailability of Cinnarizine

Oransa¹,

Boughdady²

2022

IJN

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Purpose: Cinnarizine (CIN) is a class II BSC drug, suffering from erratic bioavailability due to its pH-dependent solubility. It has preferential absorption in the stomach. In this study, new chitosan (CS) coated niosomes of CIN (CIN-loaded chitosomes) have been developed to extend the gastric retention and ameliorate CIN oral bioavailability. Methods: Various CIN-loaded niosomes were fabricated by thin-film hydration technique and fully characterized. Based on the predetermined criteria of low particle size (PS) and high entrapment efficiency percent (EE%), niosomal formulation F1 was selected and further coated with different CS concentrations. The optimized chitosomal formulation (C2) was evaluated through solid state characterization and mucoadhesive efficiency testing. It was also subjected to cytotoxicity study on Caco-2 cells; besides, in vitro drug release, stability and pharmacokinetic studies were assessed. Results: The optimized chitosomal formulation (C2) exhibited an EE% of 58.30±2.75%, PS of 440 ±13.03 nm, PDI of 0.335±0.21 and ZP of +28.1±0.10 mv. Solid state characterization results revealed the compatibility between the vesicle components and the entrapment of CIN within niosomal vesicles. C2 formulation demonstrated favorable mucoadhesive efficiency. The cytotoxicity study on Caco-2 cells manifested the safety of the optimized chitosomal formulation (C2) over the free drug. Additionally, it displayed a remarkable sustaining of CIN in vitro release up to 8 h and exhibited a good stability at the refrigerated temperature up to 3 months. In vivo pharmacokinetic assessment revealed that the CIN bioavailability from the optimized chitosomal formulation C2 was enhanced by 2.79 and 1.92 folds compared to the free drug and uncoated niosomal formulation F1, respectively. The priority of the chitosomal formulation (C2) over the niosomal one (F1) was also conferred. Conclusion: Novel formulation of chitosan coated niosomes (chitosomes) could be presented as a promising platform to improve the oral bioavailability of drugs with narrow absorption window.

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Section: Resultsmentioning

confidence: 99%

Novel Mucoadhesive Chitosomes as a Platform for Enhanced Oral Bioavailability of Cinnarizine

Oransa¹,

Boughdady²

2022

IJN

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“…The novel approach to developing a formulation with reduced administration frequency and greater residence time leads to an increase in patient compliance. Different novel formulations, including nanostructured lipid carriers (NLCs) [ 5 ], liposomes [ 6 ], niosomes [ 7 ], ocular inserts containing nanoparticles [ 8 ] and in situ gel systems [ 9 ], have been reported to increase bioavailability as well as therapeutic efficacy. These formulations have been reported to increase drug accumulation and retention at the target site [ 10 ].…”

Section: Introductionmentioning

confidence: 99%

Preparation of NLCs-Based Topical Erythromycin Gel: In Vitro Characterization and Antibacterial Assessment

Zafar

Imam

Yasir

et al. 2022

Gels

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In the present study, erythromycin (EM)-loaded nanostructured lipid carriers (NLCs) were prepared by the emulsification and ultra-sonication method. EM-NLCs were optimized by central composite design using the lipid (A), pluronic F127 (B) and sonication time (C) as independent variables. Their effects were evaluated on particle size (Y1) and entrapment efficiency (Y2). The optimized formulation (EM-NLCs-opt) showed a particle size of 169.6 ± 4.8 nm and entrapment efficiency of 81.7 ± 1.4%. EM-NLCs-opt further transformed into an in-situ gel system by using the carbopol 940 and chitosan blend as a gelling agent. The optimized EM-NLCs in situ gel (EM-NLCs-opt-IG4) showed quick gelation and were found to be stable for more than 24 h. EM-NLCs-opt-IG4 showed prolonged drug release compared to EM in situ gel. It also revealed significant high permeation (56.72%) and flux (1.51-fold) than EM in situ gel. The irritation and hydration study results depicted no damage to the goat cornea. HET-CAM results also confirmed its non-irritant potential (zero score). EM-NLCs-opt-IG4 was found to be isotonic and also showed significantly (p < 0.05) higher antimicrobial activity than EM in situ gel. The findings of the study concluded that NLCs laden in situ gel is an alternative delivery of erythromycin for the treatment of bacterial conjunctivitis.

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“…nanoemulsion gels [14] and bilosome [15], as well as transdermal matrix patches [16], have been previously studied and reported. Despite these advances, vesicular systems such as liposomes and niosomes represent an essential drug delivery system [17,18]. The advantages of niosomes over liposomes include enhanced chemical and physical stability [19], lower costs, and the easy use of surfactants [20].…”

Section: Introductionmentioning

confidence: 99%

Innovative topical niosomal gel formulation containing diclofenac sodium (niofenac)

Âkbari

Saeedi

Morteza‐Semnani

et al. 2021

Journal of Drug Targeting

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The purpose of this research was to enhance the transdermal delivery of diclofenac sodium niosomal formulations. To characterise the obtained niosomes, SEM, XRPD, DSC and ATR-FTIR were employed. The size of the niosomes increased from 158.00±6.17 to 400.87±4.99 nm when cholesterol was incorporated into the formulations. It was observed that the zeta potential of niofenac varies from -25.40±1.352 to -43.13±1.171 mV when the cholesterol percentage decreased from 2% to 0.2%. The higher entrapment efficiency percentage (63.70±0.18%) was obtained for the formulations with larger particle sizes and higher cholesterol content. The optimised niofenac formulation showed a controlled release fashion where 61.71±0.59% of the drug released within 24 h. The results showed that the value of permeated diclofenac sodium through the skin layers was higher for the niofenac gel formulation (242.3±31.11 µg/cm 2 ) compared to simple gel formulation (127.40±27.80 µg/cm 2 ). Besides, niofenac formulation outperformed the anti-inflammatory activities in the formalin test compared to the control and diclofenac simple gel group. The licking time was significantly lower in both early (40.2±7.3 s) and late stages (432.4±31.7 s) for niofenac compared to conventional formulation (early stage 130.4±8.73 s and late stage 660.6±123.73 s). This study indicates that niosomal formulations can improve drug therapeutic effects by increasing drug delivery to specific sites.

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Formulation of Chitosan Polymeric Vesicles of Ciprofloxacin for Ocular Delivery: Box-Behnken Optimization, In Vitro Characterization, HET-CAM Irritation, and Antimicrobial Assessment

Cited by 40 publications

References 41 publications

Novel Mucoadhesive Chitosomes as a Platform for Enhanced Oral Bioavailability of Cinnarizine

Novel Mucoadhesive Chitosomes as a Platform for Enhanced Oral Bioavailability of Cinnarizine

Preparation of NLCs-Based Topical Erythromycin Gel: In Vitro Characterization and Antibacterial Assessment

Innovative topical niosomal gel formulation containing diclofenac sodium (niofenac)

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