Harnessing nanotechnology for enhanced topical delivery of clindamycin phosphate

Fatima, Nasreen; Rehman, Saleha; Nabi, Bushra; Baboota, Sanjula; Ali, Javed

doi:10.1016/j.jddst.2019.101253

Cited by 20 publications

(11 citation statements)

References 47 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Here, the subcutaneous layer acts as a reservoir to deliver drug progressively to the viable dermis layer. The slower penetration of the developed formulation will also lead to reduced systemic toxicity [33,35]. The study finding that the drug resides on the top of the dermal layer confirmed an enhanced therapeutic drug profile to treat fungal infection [39,40].…”

Section: Tape Stripping Studymentioning

confidence: 76%

See 1 more Smart Citation

Development and Evaluation of Polymeric Nanosponge Hydrogel for Terbinafine Hydrochloride: Statistical Optimization, In Vitro and In Vivo Studies

et al. 2020

Self Cite

View full text Add to dashboard Cite

Terbinafine hydrochloride, although one of the prominent antifungal agents, suffers from low drug permeation owing to its hydrophobic nature. The approach of nanosponge formulation may thus help to resolve this concern. Thus, the present research was envisioned to fabricate the nanosponge hydrogel of terbinafine hydrochloride for topical delivery since nanosponge augments the skin retentivity of the drug. The optimized formulation was obtained using Box Behnken Design. The dependent and independent process parameters were also determined wherein polyvinyl alcohol (%), ethylcellulose (%), and tween 80 (%) were taken as independent process parameters and particle size, polydispersity index (PDI), and entrapment efficiency (EE) were the dependent parameters. The nanosponge was then incorporated into the hydrogel and characterized. In-vitro drug release from the hydrogel was 90.20 ± 0.1% which was higher than the drug suspension and marketed formulation. In vitro permeation potential of the developed formulation through rat skin showed a flux of 0.594 ± 0.22 µg/cm2/h while the permeability coefficient was 0.059 ± 0.022 cm/s. Nanosponge hydrogel was evaluated for non-irritancy and antifungal activity against C. albicans and T. rubrum confirming the substantial outcome. Tape stripping studies exhibited ten times stripping off the skin quantified 85.6 ± 0.21 μg/cm2. The confocal analysis justified the permeation potential of the prepared hydrogel. The mean erythemal score was 0.0, confirming that the prepared hydrogel did not cause erythema or oedema. Therefore, based on results obtained, nanosponge hydrogel formulation is a potential carrier for efficient topical delivery of terbinafine hydrochloride.

show abstract

Section: Tape Stripping Studymentioning

confidence: 76%

“…The process seems to be following the Gibbs-Thompson equation [32]. The amorphous structure of the TH-NS established by the result obtained is desirable for enhanced drug entrapment within the NS structure [33].…”

Section: Thermoanalytical Technique (Dsc)mentioning

confidence: 93%

Development and Evaluation of Polymeric Nanosponge Hydrogel for Terbinafine Hydrochloride: Statistical Optimization, In Vitro and In Vivo Studies

et al. 2020

Self Cite

View full text Add to dashboard Cite

show abstract

“…The PDI signifies the distribution of the size of the nanocarriers in the formulation. PDI values less than 0.5 signify that the formulation is monodispersed (homogeneity), whereas a PDI value more than 0.5 signifies the polydispersity of the formulation [ 60 ].…”

Section: Resultsmentioning

confidence: 99%

Thymoquinone-Enriched Naringenin-Loaded Nanostructured Lipid Carrier for Brain Delivery via Nasal Route: In Vitro Prospect and In Vivo Therapeutic Efficacy for the Treatment of Depression

et al. 2022

Self Cite

View full text Add to dashboard Cite

In the current research, a thymoquinone-enriched naringenin (NGN)-loaded nanostructured lipid carrier (NLC) was developed and delivered via the nasal route for depression. Thymoquinone (TQ) oil was used as the liquid lipid and provided synergistic effects. A TQ- and NGN-enriched NLC was developed via the ultrasonication technique and optimized using a central composite rotatable design (CCRD). The optimized NLC exhibited the following properties: droplet size, 84.17 to 86.71 nm; PDI, 0.258 to 0.271; zeta potential, −8.15 to −8.21 mV; and % EE, 87.58 to 88.21%. The in vitro drug release profile showed the supremacy of the TQ-NGN-NLC in comparison to the NGN suspension, with a cumulative drug release of 82.42 ± 1.88% from the NLC and 38.20 ± 0.82% from the drug suspension. Ex vivo permeation study displayed a 2.21-fold increase in nasal permeation of NGN from the NLC compared to the NGN suspension. DPPH study showed the better antioxidant potential of the TQ-NGN-NLC in comparison to NGN alone due to the synergistic effect of NGN and TQ oil. CLSM images revealed deeper permeation of the NGN-NLC (39.9 µm) through the nasal mucosa in comparison to the NGN suspension (20 µm). Pharmacodynamic studies, such as the forced swim test and the locomotor activity test, were assessed in the depressed rat model, which revealed the remarkable antidepressant effect of the TQ-NGN-NLC in comparison to the NGN suspension and the marketed formulation. The results signify the potential of the TQ-enriched NGN-NLC in enhancing brain delivery and the therapeutic effect of NGN for depression treatment.

show abstract

“…Clindamycin has been shown to be effective, safe, and well-tolerated after topical application, and it is currently available in a variety of different vehicles differing in the amount of water, alcohol and oil, including lotions, solutions, gels, and foams [ 8 ]. Although widely used in dermatology, the major issue of conventional clindamycin topical formulations for effective treatment is the hydrophilic nature of clindamycin (log P = 0.5), not suitable for skin penetration and accumulation in the pilosebaceous structures as lipophilic environment [ 9 , 10 ]. Clindamycin is a water-soluble weak base (pKa 7.72), which is mostly in ionized form at physiological pH [ 11 ], and it is usually classified in class III of the Biopharmaceutics Classification System (BCS), with good aqueous solubility and poor membrane permeability.…”

Section: Introductionmentioning

confidence: 99%

“…Clindamycin is a water-soluble weak base (pKa 7.72), which is mostly in ionized form at physiological pH [ 11 ], and it is usually classified in class III of the Biopharmaceutics Classification System (BCS), with good aqueous solubility and poor membrane permeability. Based on the drawbacks of clindamycin itself and its conventional formulations, several vesicular and particulate nanodelivery systems of clindamycin have been developed in order to enhance the delivery of clindamycin to the intended site of action after topical application [ 9 , 12 , 13 , 14 , 15 ].…”

Section: Introductionmentioning

confidence: 99%

Influence of Bile Acids in Hydrogel Pharmaceutical Formulations on Dissolution Rate and Permeation of Clindamycin Hydrochloride

Pavlović

Bogićević

Zaklan

et al. 2022

Gels

View full text Add to dashboard Cite

Clindamycin hydrochloride is a widely used antibiotic for topical use, but its main disadvantage is poor skin penetration. Therefore, new approaches in the development of clindamycin topical formulations are of great importance. We aimed to investigate the effects of the type of gelling agent (carbomer and sodium carmellose), and the type and concentration of bile acids as penetration enhancers (0.1% and 0.5% of cholic and deoxycholic acid), on clindamycin release rate and permeation in a cellulose membrane in vitro model. Eight clindamycin hydrogel formulations were prepared using a 23 full factorial design, and they were evaluated for physical appearance, pH, drug content, drug release, and permeability parameters. Although formulations with carbomer as the gelling agent exerted optimal sensory properties, carmellose sodium hydrogels had significantly higher release rates and permeation of clindamycin hydrochloride. The bile acid enhancement factors were higher in carbomer gels, and cholic acid exerted more pronounced permeation-enhancing effects. Since the differences in the permeation parameters of hydrogels containing cholic acid in different concentrations were insignificant, its addition in a lower concentration is more favorable. The hydrogel containing carmellose sodium as a gelling agent and 0.1% cholic acid as a penetration enhancer can be considered as the formulation of choice.

show abstract

Harnessing nanotechnology for enhanced topical delivery of clindamycin phosphate

Cited by 20 publications

References 47 publications

Development and Evaluation of Polymeric Nanosponge Hydrogel for Terbinafine Hydrochloride: Statistical Optimization, In Vitro and In Vivo Studies

Development and Evaluation of Polymeric Nanosponge Hydrogel for Terbinafine Hydrochloride: Statistical Optimization, In Vitro and In Vivo Studies

Thymoquinone-Enriched Naringenin-Loaded Nanostructured Lipid Carrier for Brain Delivery via Nasal Route: In Vitro Prospect and In Vivo Therapeutic Efficacy for the Treatment of Depression

Influence of Bile Acids in Hydrogel Pharmaceutical Formulations on Dissolution Rate and Permeation of Clindamycin Hydrochloride

Contact Info

Product

Resources

About