Enhancement of oral bioavailability of anti-HIV drug rilpivirine HCl through nanosponge formulation

Zainuddin, Rana; Zaheer, Zahid; Sangshetti, Jaiprakash N.; Momin, Mufassir Mushtaque

doi:10.1080/03639045.2017.1371732

Cited by 49 publications

(33 citation statements)

References 31 publications

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“…to Higuchi-Connors release kinetic model (R 2 = 0.995) indicating that drug release was carried out by diffusion from the nanosponges (Machín, Isasi, & Vélaz, 2012;Zainuddin, Zaheer, Sangshetti, & Momin, 2017).…”

Section: (A) (B)mentioning

confidence: 99%

Evaluation of solubility enhancement, antioxidant activity, and cytotoxicity studies of kynurenic acid loaded cyclodextrin nanosponge

Dhakar

Caldera

Bessone

et al. 2019

Carbohydrate Polymers

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The aqueous solubility of KYNA was increased by encapsulation with β-CDNS2. • The molar ratio of CDI to β-CD affected the solubilization efficiency of nanosponges. • Higher antioxidant activity of KYNA loaded NS was achieved compared to plain KYNA. • Cell viability study showed that NS was nontoxic to SHSY-5Y human neuroblastoma cell lines. • The particle size and zeta potential of KYNA loaded NS and blank NS remained unchanged on storage.

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Section: (A) (B)mentioning

confidence: 99%

Evaluation of solubility enhancement, antioxidant activity, and cytotoxicity studies of kynurenic acid loaded cyclodextrin nanosponge

Dhakar

Caldera

Bessone

et al. 2019

Carbohydrate Polymers

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“…Biodegradability, biocompatibility, stability in the pH of 1–11 and negligible toxicity of NSs rendered them as safe drug carriers . To date, NSs have been used for delivery of various drugs such as Rilpivirine, Rosuvastatin calcium, Acyclovir, Norfloxacin, Anti‐restenotic Agent DB103, Doxorubicin and Captopril, Efavirenz, Nifedipine, Camptothecin, Paclitaxel and Curcumin …”

Section: Introductionmentioning

confidence: 99%

“…[12][13][14][15][16][17][18][19][20][21][22] Biodegradability, biocompatibility, stability in the pH of 1-11 and negligible toxicity of NSs rendered them as safe drug carriers. [23] To date, NSs have been used for delivery of various drugs such as Rilpivirine, [24,25] Rosuvastatin calcium, [26] Acyclovir, [27] Norfloxacin, [28] Anti-restenotic Agent DB103, [29] Doxorubicin and Captopril, [30] Efavirenz, [31] Nifedipine, [32] Camptothecin, [33] Paclitaxel [34] and Curcumin. [35] Diferuloylmethane (Curcumin), important bioactive component, is a natural phenolic compound derived from the spice turmeric (Curcuma longa).…”

Section: Introductionmentioning

confidence: 99%

Cyclodextrin‐Based Nanosponges for Improving Solubility and Sustainable Release of Curcumin

et al. 2020

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Considering the utility of cyclodextrin nanosponges for the encapsulation of drugs, in this study, the effect of drug loading method on the release property of the resulting complex is studied. To this purpose, curcumin as a model substrate was loaded into the cyclodextrin nanosponge via three different methods, including freeze drying, impregnation and physical mixing.All three complexes were characterized and the release profile of curcumin from them was investigated.[a] M. Gharakhloo, M. Rezaeetabar, Dr. A. Rahimi

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“…Ideally, an anti‐HIV drug should have a satisfactory oral bioavailability and a suitable elimination half‐life, allowing low frequent oral treatment and low dosages. RPV (Figure 2) has a relatively long elimination half‐life ( t 1/2 = 45 h) and the RPV·HCl (RLP) has an acceptable oral bioavailability ( F = 32%) 100 . However, with comparison of its high in vitro potency, the original form of RPV was limited by the poor solubility and the F values could not be accurately measured which was pH dependent 101 .…”

Section: Improvement Of Pk Profilesmentioning

confidence: 99%

Druggability modification strategies of the diarylpyrimidine‐type non‐nucleoside reverse transcriptase inhibitors

Zhuang

Chen

2021

Medicinal Research Reviews

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Drug discovery of human immunodeficiency virus (HIV) is a hot field in medicinal chemistry community for many years. The diarylpyrimidines (DAPYs) are the second‐generation non‐nucleoside reverse transcriptase inhibitors (NNRTIs) targeting reverse transcriptase, playing a great irreplaceable role in HIV transcriptional therapy. However, fast‐growing drug‐resistant mutations as nonnegligible challenge are still unpredictably appeared in the clinical practice, leading to deactivate or reduce the existing drugs. In the last 20 years, more and more novel DAPY derivatives have developed with the purpose to counter the mutants. Nevertheless, most of them have dissatisfactory pharmacokinetics (PK) or poor antiviral activity toward resistant mutant strains. In this article, we will analyze the NNRTI derivatives with promising druggability, and summarize a series of druggability modification strategies to improve the antiviral activity, reduce toxicity and improve the PK properties in recent years. The prospects of DAPYs and the directions for future efforts will be discussed.

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Enhancement of oral bioavailability of anti-HIV drug rilpivirine HCl through nanosponge formulation

Abstract: The approach offers a comfortable dosing zone for AIDs patients, negating the requirement of consuming the formulation in a fed state due to enhancement in drugs' oral bioavailability.

Cited by 49 publications

References 31 publications

Evaluation of solubility enhancement, antioxidant activity, and cytotoxicity studies of kynurenic acid loaded cyclodextrin nanosponge

Evaluation of solubility enhancement, antioxidant activity, and cytotoxicity studies of kynurenic acid loaded cyclodextrin nanosponge

Cyclodextrin‐Based Nanosponges for Improving Solubility and Sustainable Release of Curcumin

Druggability modification strategies of the diarylpyrimidine‐type non‐nucleoside reverse transcriptase inhibitors

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