Development of thermosensitive and mucoadhesive gels of cabotegravir for enhanced permeation and retention profiles in vaginal tissue: A proof of concept study

Enggi, Cindy Kristina; Isa, Hansel Tridatmojo; Sulistiawati, Sulistiawati; Ardika, Komang Agus Rai; Wijaya, Stevens; Asri, Rangga Meidianto; Mardikasari, Sandra Aulia; Donnelly, Ryan F.; Permana, Andi Dian

doi:10.1016/j.ijpharm.2021.121182

Cited by 25 publications

(20 citation statements)

References 38 publications

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“…As positive and negative controls, PBS and water were also measured, respectively. The percentage of hemolytic activity was calculated through the equation below , hemolysis 0.25em ( % ) = ( Ab s test sample − Ab s negative control Ab s test sample − Ab s negative control ) × 100 % …”

Section: Methodsmentioning

confidence: 99%

“…The right pan of a double-pan was added with loads every 30 s over the pan to measure the maximum weight required to detach the hydrogel from the skin tissue. The bioadhesive strength was calculated in terms of force per unit area using the following equation , b ioadhesive strength 0.25em ( N / m 2 ) = 0.25em m × g × 0.1 A where m is the weight (g) required to remove the formed hydrogel from the rat skin, g is the gravity acceleration (9.8 m/s 2 ), and A is the surface area of the rat skin (cm 2 ).…”

Section: Methodsmentioning

confidence: 99%

“…As positive and negative controls, PBS and water were also measured, respectively. The percentage of hemolytic activity was calculated through the equation below 47,48 In vitro release studies were conducted by the dialysis membrane diffusion technique. Briefly, the dispersion was sealed into Spectra-Por, a 12,000−14,000 MWCO dialysis membrane bag (Spectrum Medical Industries, Los Angeles, CA).…”

Section: Extraction Processmentioning

confidence: 99%

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Development of Solid Lipid Nanoparticle-Loaded Polymeric Hydrogels Containing Antioxidant and Photoprotective Bioactive Compounds of Safflower (Carthamus tinctorius L.) for Improved Skin Delivery

et al. 2023

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Safflower (Carthamus tinctorius L.) is a potent natural antioxidant because of active compounds such as quercetin (QU) and luteolin (LU). These components prevent damage to the skin caused by free radicals from UV rays. However, due to the poor solubility and transdermal permeation, the effectiveness of the compounds in showing their activity was limited. In this study, we develop solid lipid nanoparticle (SLN)-based hydrogel formulations to enhance the solubility and penetration of two bioactive compounds found in safflower petals extract (SPE). The hot emulsification-ultrasonication method was used to produce SLNs, and to obtain high antioxidant activity, 100% v/v ethanol was used in the extraction procedure. The results showed that this approach could encapsulate >80% of both QU and LU. Moreover, Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) spectra indicated that most of the QU and LU were trapped in a lipid matrix and dispersed homogeneously at the molecular level, increasing the solubility. Additionally, SLN-hydrogel composites are able to release two lipophilic bioactive compounds for 24 h, which also demonstrated increased skin retention and penetrability of the QU and LU up to 19-fold. In vitro blood biocompatibility showed that no hemolytic toxicity was observed below 500 μg/mL. Accordingly, the formulation was considered safe for use. Sun protective factor (SPF) test shows a value above 15, showing an excellent promising application as the photoprotective agent to prevent symptoms associated with photoinduced skin aging.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Extraction Processmentioning

confidence: 99%

See 1 more Smart Citation

Development of Solid Lipid Nanoparticle-Loaded Polymeric Hydrogels Containing Antioxidant and Photoprotective Bioactive Compounds of Safflower (Carthamus tinctorius L.) for Improved Skin Delivery

et al. 2023

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“…For instance, a significant increase in drug permeation was observed with a vaginal in situ gel formulation of fluconazole, which could be attributed to both the improved drug release profile of the drug in the formulation as well as the interaction between chitosan used in the formulation and mucin present in the vaginal mucosal layer [ 163 ]. Studies on VDDS report an increase in drug permeability by the use of polyethylene glycol [ 164 ].…”

Section: Sol–gel Platform Technology In Vaginal Drug Delivery Systemmentioning

confidence: 99%

“…For instance, in a study comprising a thermosensitive formulation, mucoadhesive formulation, and thermosensitive–mucoadhesive system, the in situ mucoadhesive gel was considered the optimum formulation, with a longer vaginal residence time compared to the two other systems (>8 h). The study suggests that both gelation and mucoadhesiveness together result in a robust vaginal formulation [ 164 ].…”

Section: Sol–gel Platform Technology In Vaginal Drug Delivery Systemmentioning

confidence: 99%

Application of Sol–Gels for Treatment of Gynaecological Conditions—Physiological Perspectives and Emerging Concepts in Intravaginal Drug Delivery

Thapa

Gurung

Parat

et al. 2022

Gels

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Approaches for effective and sustained drug delivery to the female reproductive tract (FRT) for treating a range of gynaecological conditions remain limited. The development of versatile delivery platforms, such as soluble gels (sol–gels) coupled with applicators/devices, holds considerable therapeutic potential for gynaecological conditions. Sol–gel systems, which undergo solution-to-gel transition, triggered by physiological conditions such as changes in temperature, pH, or ion composition, offer advantages of both solution- and gel-based drug formulations. Furthermore, they have potential to be used as a suitable drug delivery vehicle for other novel drug formulations, including micro- and nano-particulate systems, enabling the delivery of drug molecules of diverse physicochemical character. We provide an anatomical and physiological perspective of the significant challenges and opportunities in attaining optimal drug delivery to the upper and lower FRT. Discussion then focuses on attributes of sol–gels that can vastly improve the treatment of gynaecological conditions. The review concludes by showcasing recent advances in vaginal formulation design, and proposes novel formulation strategies enabling the infusion of a wide range of therapeutics into sol–gels, paving the way for patient-friendly treatment regimens for acute and chronic FRT-related conditions such as bacterial/viral infection control (e.g., STDs), contraception, hormone replacement therapy (HRT), infertility, and cancer.

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Lipid Complex-Itraconazole in Thermosensitive Mucoadhesive Vaginal Gel to Enhance the Effectiveness of Therapy for Vulvovaginal Candidiasis: Formulation, Optimization, Characterization, and Ex vivo Evaluation

et al. 2023

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Development of thermosensitive and mucoadhesive gels of cabotegravir for enhanced permeation and retention profiles in vaginal tissue: A proof of concept study

Cited by 25 publications

References 38 publications

Development of Solid Lipid Nanoparticle-Loaded Polymeric Hydrogels Containing Antioxidant and Photoprotective Bioactive Compounds of Safflower (Carthamus tinctorius L.) for Improved Skin Delivery

Development of Solid Lipid Nanoparticle-Loaded Polymeric Hydrogels Containing Antioxidant and Photoprotective Bioactive Compounds of Safflower (Carthamus tinctorius L.) for Improved Skin Delivery

Application of Sol–Gels for Treatment of Gynaecological Conditions—Physiological Perspectives and Emerging Concepts in Intravaginal Drug Delivery

Lipid Complex-Itraconazole in Thermosensitive Mucoadhesive Vaginal Gel to Enhance the Effectiveness of Therapy for Vulvovaginal Candidiasis: Formulation, Optimization, Characterization, and Ex vivo Evaluation

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