To study the impact of exposure to electromagnetic fields on the permeability of saquinavir (drug in AIDS therapy) across the blood-brain barrier. Effects of systematic parameters of electromagnetic fields (power, wave types, frequency, modulation) were especially examined.
Transport of anti-retroviral agents across the blood-brain barrier is of key importance for the treatment of the acquired immunodeficiency syndrome (AIDS): Saquinavir is a protease inhibitor for reducing enzymatic activity and inducing immature filial generation of HIV (anti-human immunodeficiency virus). That is, saquinavir medication generates non-infectious virus to obtain therapeutical effect in the AIDS therapy. Transport of HIV agents across the blood-brain barrier is a prerequisite for the treatment of AIDS because HIV is replicated in the brain of HIV-infected individuals.
As pharmaceutical strategy for drug delivery, saquinavir was incorporated with PBCA (polybutylcyanoacrylate), MMA-SPM (methylmethacrylate-sulfopropylmethacrylate), and SLN (solid lipid nanoparticle).
| Exposure | Parameters |
|---|---|
|
Exposure 1:
0–915 MHz
Modulation type:
CW
Exposure duration:
continuous for 90 min
|
|
|
Exposure 2:
915 MHz
Modulation type:
AM
Exposure duration:
continuous for 90 min
|
|
|
Exposure 3:
915 MHz
Modulation type:
FM
Exposure duration:
continuous for 90 min
|
|
|
Exposure 4:
915 MHz
Modulation type:
CW
Exposure duration:
continuous for 90 min
|
| Frequency | 915 MHz |
|---|---|
| Type | |
| Exposure duration | continuous for 90 min |
| Modulation type | AM |
|---|---|
| Modulation frequency | 20 MHz |
| Modulation depth | 100 % |
| Additional info |
sine, square, or triangle wave |
| Exposure source |
|
|---|
| Measurand | Value | Type | Method | Mass | Remarks |
|---|---|---|---|---|---|
| power | 5 mW | - | - | - | - |
| Frequency | 915 MHz |
|---|---|
| Type | |
| Exposure duration | continuous for 90 min |
| Modulation type | FM |
|---|---|
| Modulation frequency | 20 MHz |
| Additional info |
sine or square wave, deviation 400 kHz |
| Exposure source |
|
|---|
| Measurand | Value | Type | Method | Mass | Remarks |
|---|---|---|---|---|---|
| power | 5 mW | - | - | - | - |
| Frequency | 915 MHz |
|---|---|
| Type | |
| Exposure duration | continuous for 90 min |
| Modulation type | CW |
|---|
| Exposure source |
|
|---|---|
| Additional info | This exposure was for testing cell viability and other effects. |
High power of electromagnetic fields caused apoptosis and power of 5 mW was apposite for the investigation on human brain-microvascular endothelial cells without obvious apoptosis.
Square wave produced greater permeability than sinusoidal and triangle waves. The carrier order on permeability of saquinavir across the blood-brain barrier model under exposure was SLN>PBCA>MMA-SPM. Also, a larger frequency, modulation or depth of amplitude modulation (AM), or modulation or deviation of frequency modulation (FM) yielded a greater permeability. Besides, enhancement of permeability by AM wave was more significant than that by FM wave.
Transport behaviour of saquinavir across the blood-brain barrier model was strongly influenced by the combination of nanoparticulate PBCA, MMA-SPM, and SLN with electromagnetic field exposure. This combination would be beneficial to the clinical application to the therapy of AIDS and other brain-related diseases.
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