Polymeric hydrogel forming microneedle-mediated transdermal delivery of sildenafil citrate from direct-compressed tablet reservoir for potential improvement of pulmonary hypertension therapy

Fitri, Andi Maqhfirah Nurul; Elim, Diany; Mahfud, Muhammad Alif Sya'ban; Sultan, Nurul Aisha Fitri; Saputra, Mesakh Diki; Afika, Nur; Friandini, Rissa Ardita; Djide, Natsir; Permana, Andi Dian

doi:10.1016/j.ijpharm.2022.122549

Cited by 17 publications

(22 citation statements)

References 70 publications

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“…Enhanced swelling capacity leads to improved drug permeation profiles, as supported by a previous study. 33 Furthermore, the gel fraction percentage was found to be 78.07 ± 6.57% for F1-110-80 and 75.70 ± 1.64% for F3-80-120. The gel fraction represents the cross-linked portion of the hydrogel, and a highly cross-linked hydrogel with a denser structure and a smaller mesh size can impede analyte movement due to limited diffusion space within the swollen hydrogel.…”

Section: Preparation and Physicalmentioning

confidence: 95%

“…The spectra were recorded over the range of 4000−500 cm −1 at a resolution of 2 cm −1 . 33 2.9. Thermal Analysis of HFMN.…”

Section: Mechanical and Insertionmentioning

confidence: 99%

“…This was coupled with an increased intensity at ∼1735 cm −1 , suggesting enhanced formation of the ester group. 19,33 3.6. Thermal Analysis of HFMN.…”

Section: Mechanical and Insertion Properties Of Hfmnmentioning

confidence: 99%

“…91 In addition, only R1, R2, and R3 exhibit the desired tablet hardness (∼30 N/ cm 2 ). 33 Figure 10C shows the dissolution time of the DCT reservoir. The DCT reservoirs exhibit dissolution times of 73.33 ± 2.52, 57.33 ± 3.51, 30.67 ± 2.08, 27.67 ± 1.53, and 21.33 ± 2.52 s for R1, R2, R3, R4, and R5, respectively.…”

Section: Preparation and Physicalmentioning

confidence: 99%

“…More intramolecular and intermolecular bonds were formed in the structure of hydrogels at an increased cross-linking time and temperature, which is responsible for the improvement in the mechanical strength of HFMN. 33 Nevertheless, all formulations showed a height reduction percentage below 10%, which is considered adequate to withstand a compression force. 64 The insertion properties of HFMN were determined by calculating the number of parafilm layers successfully penetrated after testing.…”

Section: Mechanical and Insertion Properties Of Hfmnmentioning

confidence: 99%

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Application of Biomaterials in the Development of Hydrogel-Forming Microneedles Integrated with a Cyclodextrin Drug Reservoir for Improved Pharmacokinetic Profiles of Telmisartan

Enggi,

Sulistiawati,

Himawan

et al. 2024

ACS Biomater. Sci. Eng.

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However, its oral application is limited by its poor water solubility. This study presents the successful utilization of biomaterial-based hydrogelforming microneedles integrated with a direct compressed tablet reservoir (HFMN-DCT) for the transdermal delivery of telmisartan in the treatment of hypertension. The combination of PVP, PVA, and tartaric acid was used in the HFMN formulation. A range of cross-linking temperatures and times were employed to optimize the characteristics of the HFMN. The HFMN exhibited excellent swelling capacity, mechanical strength, and insertion properties. Additionally, the poorly soluble characteristic of TEL was improved by the inclusion complex formulation with β-cyclodextrin (βCD). Phase solubility analysis showed an A p -type diagram, indicating a higher-order complex between TEL and βCD, with respect to βCD. A ratio of TEL:βCD of 1:4 mM demonstrates the highest solubility enhancement of TEL. The inclusion complex formation was confirmed by FTIR, XRD, DSC, and molecular docking studies. A significantly higher release of TEL (up to 20-fold) from the inclusion complex was observed in the in vitro release study. Subsequently, a DCT reservoir was developed using various concentrations of sodium starch glycolate. Essentially, both the HFMN and DCT reservoir exhibit hemocompatibility and did not induce any skin irritation. The optimized combination of the HFMN-DCT reservoir showed an ex vivo permeation profile of 83.275 ± 2.405%. Notably, the proposed system showed superior pharmacokinetic profiles in the in vivo investigation using male Wistar rats. Overall, this study highlights the potential of HFMN-DCT reservoir systems as a versatile platform for transdermal drug delivery applications.

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Section: Preparation and Physicalmentioning

confidence: 95%

“…The spectra were recorded over the range of 4000−500 cm −1 at a resolution of 2 cm −1 . 33 2.9. Thermal Analysis of HFMN.…”

Section: Mechanical and Insertionmentioning

confidence: 99%

“…This was coupled with an increased intensity at ∼1735 cm −1 , suggesting enhanced formation of the ester group. 19,33 3.6. Thermal Analysis of HFMN.…”

Section: Mechanical and Insertion Properties Of Hfmnmentioning

confidence: 99%

Section: Preparation and Physicalmentioning

confidence: 99%

Section: Mechanical and Insertion Properties Of Hfmnmentioning

confidence: 99%

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Application of Biomaterials in the Development of Hydrogel-Forming Microneedles Integrated with a Cyclodextrin Drug Reservoir for Improved Pharmacokinetic Profiles of Telmisartan

Enggi,

Sulistiawati,

Himawan

et al. 2024

ACS Biomater. Sci. Eng.

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Application of hydrogel microneedles in the oral cavity

He,

Fan

et al. 2024

Biopolymers

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Microneedles are a transdermal drug delivery system in which the needle punctures the epithelium to deliver the drug directly to deep tissues, thus avoiding the influence of the first‐pass effect of the gastrointestinal tract and minimizing the likelihood of pain induction. Hydrogel microneedles are microneedles prepared from hydrogels that have good biocompatibility, controllable mechanical properties, and controllable drug release and can be modified to achieve environmental control of drug release in vivo. The large epithelial tissue in the oral cavity is an ideal site for drug delivery via microneedles. Hydrogel microneedles can overcome mucosal hindrances to delivering drugs to deep tissues; this prevents humidity and a highly dynamic environment in the oral cavity from influencing the efficacy of the drugs and enables them to obtain better therapeutic effects. This article analyzes the materials and advantages of common hydrogel microneedles and reviews the application of hydrogel microneedles in the oral cavity.

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Selective Delivery of Clindamycin Using a Combination of Bacterially Sensitive Microparticle and Separable Effervescent Microarray Patch on Bacteria Causing Diabetic Foot Infection

Fauziah,

Safirah,

Rahmadani

et al. 2024

Pharm Res

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Polymeric hydrogel forming microneedle-mediated transdermal delivery of sildenafil citrate from direct-compressed tablet reservoir for potential improvement of pulmonary hypertension therapy

Cited by 17 publications

References 70 publications

Application of Biomaterials in the Development of Hydrogel-Forming Microneedles Integrated with a Cyclodextrin Drug Reservoir for Improved Pharmacokinetic Profiles of Telmisartan

Application of Biomaterials in the Development of Hydrogel-Forming Microneedles Integrated with a Cyclodextrin Drug Reservoir for Improved Pharmacokinetic Profiles of Telmisartan

Application of hydrogel microneedles in the oral cavity

Selective Delivery of Clindamycin Using a Combination of Bacterially Sensitive Microparticle and Separable Effervescent Microarray Patch on Bacteria Causing Diabetic Foot Infection

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