Drug name
Last update: Apr 2026Bictegravir-PLGA nanoformulation
Developer(s)
Drug information
Bictegravir
Bictegravir PLGA nanoformulation
Small molecule
Second-generation Integrase Strand Transfer Inhibitors (INSTI)
Bictegravir (BIC), an HIV‑1 integrase strand transfer inhibitor, was successfully formulated into <200 nm poly(lactic‑co‑glycolic acid) (PLGA) nanoparticles using an o/w emulsion–solvent evaporation technique. The formulation achieved an encapsulation efficiency of 47.9 ± 6.9% and exhibited a stable negative surface charge (zeta potential approximately −23 mV). In TZM‑bl cell assays, nanoencapsulation markedly enhanced antiviral potency, reducing the EC50 from 0.604 µM for free BIC to 0.0038 µM, while increasing the CC50 to 820.4 µM, resulting in a selectivity index of ~ 215,900; Cmax -888.54 pmole. The nanoparticles demonstrated sustained intracellular retention in PBMCs for up to 28 days. Following single preclinical SC dose, BIC had sustained plasma and tissue drug levels for >30 days.
Not approved for clinical use yet.
Not approved for clinical use yet.
Therapeutic area(s)
- HIV
- Treatment
Administration route
Subcutaneous
Associated long-acting platforms
Polymer-based particles
Use of drug
- Administered by a community health worker
- Administered by a nurse
- Administered by a specialty health worker
Not provided
Not provided
Dosage
0.0002225 µM– 44.5 µM (preclinical doses)
44.5 µM
Not applicable for preclinical studies
Not provided
Not provided
Comment & Information
Developer(s)
Creighton University
Creighton University, founded in 1878 in Omaha by the Creighton family, is a Jesuit institution known for academic excellence, healthcare education, and service. It supports research in drug discovery and medical innovation, with strong science and pharmacy programs. Its modern campuses, labs, libraries, and clinical facilities help drive learning and community impact.
Drug structure
Scale-up and manufacturing prospects
Not known
1. High‑shear emulsification 2. Nano‑emulsification 3. Biosafety handling 4. Solvent evaporation 5. Drying 6. Temperature control 7. Centrifugation (release testing) 8. Probe sonicator 9. Orbital shaker
Oil‑in‑water (O/W) emulsion–solvent evaporation methodology:- i) 5 mL DCM containing PLGA, Poloxamer 407 and BIC (10:10:2 w:w:w) added dropwise to 20 mL of 1 % PVA solution under high‑speed continuous stirring. iii) Mixing PLGA (75:25 lactide:glycolide; MW 4000–15000), luronic F127 (stabilizer), polyvinyl alcohol aqueous phase, dichloromethane organic phase iv) Dissolve BIC to form solution v) Form homogeneous phase of solution vi) Emulsification process: Emulsify solution to form o/w emulsion with PLGA mixture v) Evaporate o/w emulsion to form encapsulated BIC.
1. Dynamic light scattering (DLS) 2. ZetaPlus Zeta Potential Analyzer 3. Hitachi S‑4700 field‑emission Scanning Electron Microscope (SEM) 4. High performance liquid chromatography (HPLC) 5. Liquid chromatography-Mass Spectrometry (LCMS)
Excipients
Not provided
(i) PLGA (ii) Poloxamer 407
Not provided
Delivery device(s)
No delivery device
Nanoparticles and methods of use
Provided herein are nanoparticles and methods for using nanoparticles. The nanoparticles include at least three antiretroviral agents. When introduced to cells the nanoparticles cause an increase in the intracellular concentration of the antiretroviral agents to a level that is at least the IC50 against HIV-I or HIV-2. This concentration may be maintained for at least 21 days after the cells are contacted with the nanoparticle. When administered to a subject the nanoparticles cause the concentration of the antiretroviral agents to increase to at least 100 ng/ml in the serum of the subject, at least 0.5 μg/gram tissue in an organ of the subject, or a combination thereof. Such a concentration may be maintained for at least 21 days after the administration.
US8846096B2
Not provided
Creighton University
Not provided
January 25, 2030
Active
Encapsulation of hydrophillic antiretroviral drugs in nanocarriers
An encapsulated hydrophilic antiretroviral drug including a biodegradable polymeric nanoparticle and a process for fabricating biodegradable polymeric nanoparticles to encapsulate hydrophilic antiretroviral drugs are described. In an implementation, an encapsulated hydrophilic antiretroviral drug including a biodegradable polymeric nanoparticle includes a hydrophilic antiretroviral drug; and a biodegradable polymer polymeric nanoparticle that encapsulates the hydrophilic antiretroviral drug to form a nano-sized encapsulated hydrophilic antiretroviral drug.
US20150374639A1
Not provided
Creighton University
Not provided
Not provided
Abandoned
Publications
Mandal, S., Prathipati, P. K., Belshan, M., & Destache, C. J. (2019). A potential long-acting bictegravir loaded nano-drug delivery system for HIV-1 infection: A proof-of-concept study. Antiviral research, 167, 83–88. https://doi.org/10.1016/j.antiviral.2019.04.007
Bictegravir (BIC), a newly FDA-approved integrase strand transfer inhibitor (INSTI), as a single tablet regimen has proven efficacious in treating HIV-1 and SIV viruses, with reduced resistance. BIC clinical trials have not investigated its prophylaxis potency. This study investigates the HIV prevention potency of a novel long-acting BIC nano-formulation aimed to improve adherence. Poly (lactic-co-glycolic acid) loaded BIC nanoparticles (BIC NPs) were formulated using an oil-in-water emulsion methodology. BIC NPs were <200 nm in size, with 47.9 ± 6.9% encapsulation efficiency. A novel, sensitive and high throughput LC-MS/MS method was used to estimate intracellular pharmacokinetics (PK) of BIC NPs and compared to BIC solution demonstrated prolonged intracellular BIC retention. BIC NPs safety was assessed based on cytotoxicity. Further, in-vitro prevention study of BIC NPs vs BIC solution was assessed against HIV-1NLX and HIV-1ADA on TZM-bl cell line and PBMCs, respectively. BIC nanoencapsulation demonstrated elevated cellular cytotoxicity concentration (CC50: 2.25 μM (BIC solution) to 820.4 μM (BIC NPs)] and lowers HIV-1 inhibitory concentration [EC50: 0.604 μM (BIC solution) to 0.0038 μM (BIC NPs)) thereby improving selectivity index (SI) from 3.7 (BIC solution) to 215,789 (BIC NP) for TZM-bl cells. Comparable results in PBMCs were obtained where BIC NPs improved SI from 0.29 (BIC solution) to 523.33 (BIC NPs). This demonstrates long-acting BIC nano-formulation with sustained drug-release potency, improved BIC cytotoxicity and enhanced HIV-1 protection compared to BIC in solution.
Additional documents
No documents were uploaded
Useful links
There are no additional links
Collaborate for development
Consider on a case by case basis, collaborating on developing long acting products with potential significant public health impact, especially for low- and middle-income countries (LMICs), utilising the referred to long-acting technology
Share technical information for match-making assessment
Provide necessary technical information to a potential partner, under confidentiality agreement, to enable preliminary assessment of whether specific medicines of public health importance in LMICs might be compatible with the referred to long-acting technology to achieve a public health benefit
Work with MPP to expand access in LMICs
In the event that a product using the referred to long-acting technology is successfully developed, the technology IP holder(s) will work with the Medicines Patent Pool towards putting in place the most appropriate strategy for timely and affordable access in low and middle-income countries, including through licensing