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Captopril (1-(2S)-3-mercapto-2-methyl-propionyl]-1-proline)
is an angiotensin-converting enzyme (ACE) inhibitor that has
been extensively used for the treatment of hypertension and congestion heart failure. According to the drug bank https://www.
drugbank.ca/drugs/DB01197 it is water soluble (4.52 mg/mL)
with logP to range between 0.34 and 1.02 based on the sources
and becomes unstable as the pH becomes greater than 1.2. This
fact decreases the therapeutic effect of captopril [3].
For this reason there have been important advances in the area
of pharmananotechnology and the controlled release of drugs,
destined to circumvent many limitations of conventional therapies
for the treatment of diseases such as hyperlipidemia, hypertension,
myocardial infarction, stroke, and thrombosis [4]. Captopril,
according to Biopharmaceutical Classification System (BCS), is a
class II drug, with high solubility but poor permeability. Thus, it is
bioconjugated with a light subunit of Agaricus bisporus mushroom
tyrosinase, a drug carrier, and for oral delivery [5]. Biodegradable
hydrogels for its controlled delivery are used [6]. Optimization of
self-nanoemulsifying orodispersible films (SNEODF) of captopril
for hypertension was studied [7]. Captopril was coated with magnetic nanoparticles (MNPs) as a new dual-mode agent for simultaneous MRI contrast and drug delivery system [8]. Gastro-retentive
captopril-loaded alginate beads were prepared by an ionotropic
gelation method using sodium alginate in combination with natural gums containing galactomannans (Senna tora, seed gum, guar
gum, and locust bean gum) in the presence of calcium chloride.
The objective of this work is to develop successful formulation of
gastro-retentive mucoadhesive alginate beads of captopril with
galactomannan [9]. Captopril-polyethyleneimine (CP) containing
low-molecular-weight polyethyleneimine and antiangiogenesis
drug captopril conjugated via an amide bond was fabricated to
modify gold nanoparticles and complex with siRNA to construct
siRNA/CP/GNP complexes for the co-delivery of drug and
siRNA in antiangiogenesis breast cancer therapy [10]. Captopril
was engulfed in a cyclodextrin-based nanosponge for studying as a
potential delivery system [11]. Due to its narrow absorption window, captopril has to be administered to the upper parts of the
intestine in order to maintain sustained therapeutic levels. Thus, it
was examined if this could be achieved by gastro-retentive dosage
form (GRDF) which consists of a drug-loaded bilayer polymeric
film, folded into a hard gelatin capsule [12]. Systematic studies
were achieved with captopril-loaded polyester fiber mats [13] and
poly(L-lactic acid/captopril) composite monofiber membranes
prepared by electrospinning and in order to increase its delivery
[14]. The intercalation of captopril (CP) into the interlayers of
montmorillonite (MMT) affords an intestine-selective drug
delivery system [15]. Methocel and Eudragit RS were used in
captopril- loaded microspheres as release-controlling factors to
Evangelia Soumelidou et al.
Captopril (1-(2S)-3-mercapto-2-methyl-propionyl]-1-proline)
is an angiotensin-converting enzyme (ACE) inhibitor that has
been extensively used for the treatment of hypertension and congestion heart failure. According to the drug bank https://www.
drugbank.ca/drugs/DB01197 it is water soluble (4.52 mg/mL)
with logP to range between 0.34 and 1.02 based on the sources
and becomes unstable as the pH becomes greater than 1.2. This
fact decreases the therapeutic effect of captopril [3].
For this reason there have been important advances in the area
of pharmananotechnology and the controlled release of drugs,
destined to circumvent many limitations of conventional therapies
for the treatment of diseases such as hyperlipidemia, hypertension,
myocardial infarction, stroke, and thrombosis [4]. Captopril,
according to Biopharmaceutical Classification System (BCS), is a
class II drug, with high solubility but poor permeability. Thus, it is
bioconjugated with a light subunit of Agaricus bisporus mushroom
tyrosinase, a drug carrier, and for oral delivery [5]. Biodegradable
hydrogels for its controlled delivery are used [6]. Optimization of
self-nanoemulsifying orodispersible films (SNEODF) of captopril
for hypertension was studied [7]. Captopril was coated with magnetic nanoparticles (MNPs) as a new dual-mode agent for simultaneous MRI contrast and drug delivery system [8]. Gastro-retentive
captopril-loaded alginate beads were prepared by an ionotropic
gelation method using sodium alginate in combination with natural gums containing galactomannans (Senna tora, seed gum, guar
gum, and locust bean gum) in the presence of calcium chloride.
The objective of this work is to develop successful formulation of
gastro-retentive mucoadhesive alginate beads of captopril with
galactomannan [9]. Captopril-polyethyleneimine (CP) containing
low-molecular-weight polyethyleneimine and antiangiogenesis
drug captopril conjugated via an amide bond was fabricated to
modify gold nanoparticles and complex with siRNA to construct
siRNA/CP/GNP complexes for the co-delivery of drug and
siRNA in antiangiogenesis breast cancer therapy [10]. Captopril
was engulfed in a cyclodextrin-based nanosponge for studying as a
potential delivery system [11]. Due to its narrow absorption window, captopril has to be administered to the upper parts of the
intestine in order to maintain sustained therapeutic levels. Thus, it
was examined if this could be achieved by gastro-retentive dosage
form (GRDF) which consists of a drug-loaded bilayer polymeric
film, folded into a hard gelatin capsule [12]. Systematic studies
were achieved with captopril-loaded polyester fiber mats [13] and
poly(L-lactic acid/captopril) composite monofiber membranes
prepared by electrospinning and in order to increase its delivery
[14]. The intercalation of captopril (CP) into the interlayers of
montmorillonite (MMT) affords an intestine-selective drug
delivery system [15]. Methocel and Eudragit RS were used in
captopril- loaded microspheres as release-controlling factors to
Evangelia Soumelidou et al.